The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27318552 |
126 |
Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study. |
Universit£ |
27364609 |
230 |
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. |
Florida A&M University |
27312422 |
219 |
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands. |
Florida A&M University |
27173799 |
97 |
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics. |
Shanghai Institute Of Materia Medica |
26954848 |
38 |
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Activea1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. |
Takeda Pharmaceutical |
26876931 |
36 |
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket. |
Abbott Healthcare Products |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
Jagiellonian University Medical College |
26900658 |
56 |
Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation. |
Jagiellonian University Medical College |
26874044 |
56 |
Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives. |
Universit£ |
26704965 |
229 |
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
University Of Illinois At Chicago |
26700945 |
68 |
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome. |
National Institute Of Biological Sciences, Beijing |
26852005 |
82 |
Novel N-acyl-carbazole derivatives as 5-HT7R antagonists. |
Yonsei University |
26698537 |
93 |
Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties. |
Jagiellonian University Medical College |
26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
26706111 |
72 |
N-Alkylated arylsulfonamides of (aryloxy)ethyl piperidines: 5-HT(7) receptor selectivity versus multireceptor profile. |
Jagiellonian University Medical College |
26271587 |
17 |
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1 F receptor agonists: Evolution from bicyclic to monocyclic cores. |
Eli Lilly |
26227779 |
37 |
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold. |
Fudan University |
26203768 |
104 |
High Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice. |
National Institute On Drug Abuse-Intramural Research Program |
25288493 |
96 |
Human alpha1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines. |
Unsw Australia |
25261823 |
107 |
Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands ata<alpha>1 and 5-HT1A receptors. |
Universit£ |
26081758 |
18 |
Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment ofß-arrestin-2. |
Karolinska Institute And Karolinska University Hospital |
25695425 |
62 |
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
City University Of New York |
25633969 |
96 |
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
University Of Illinois At Chicago |
25557493 |
109 |
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
Jagiellonian University Collegium Medicum |
25555143 |
60 |
Towards novel 5-HT7versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: design, synthesis, and antidepressant properties. Part II. |
Jagiellonian University Medical College |
25489882 |
63 |
Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase. |
Northwestern University |
25866241 |
88 |
Fingerprint-based consensus virtual screening towards structurally new 5-HT(6)R ligands. |
Jagiellonian University |
25759032 |
55 |
Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT1A and 5-HT7 receptor ligands. |
Universit£ |
25128671 |
65 |
Structure-activity relationships and molecular modeling studies of novel arylpiperazinylalkyl 2-benzoxazolones and 2-benzothiazolones as 5-HT(7) and 5-HT(1A) receptor ligands. |
Universit£ |
25127461 |
36 |
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression. |
Yonsei University |
25073094 |
24 |
The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo. |
Universidad Complutense De Madrid |
25070422 |
126 |
Further evaluation of the tropane analogs of haloperidol. |
Florida A&M University |
25556097 |
70 |
Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands. |
Washington University |
25343529 |
221 |
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
Universit£ |
25308766 |
56 |
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles. |
Chinese Academy Of Sciences |
25241924 |
47 |
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor. |
Novartis Institutes For Biomedical Research |
25182564 |
38 |
Synthesis and evaluation of arylpiperazines derivatives of 3,5-dioxo-(2H,4H)-1,2,4-triazine as 5-HT1AR ligands. |
Stony Brook University |
24878222 |
50 |
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors. |
Pfizer |
24805037 |
380 |
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. |
Adamed |
24800940 |
146 |
Identification of a new selective dopamine D4 receptor ligand. |
Florida A&M University |
24900840 |
35 |
Enhancing a CH-? Interaction to Increase the Affinity for 5-HT1A Receptors. |
University Of Li£Ge |
24559051 |
141 |
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
Intra-Cellular Therapies |
24691057 |
62 |
SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives. |
Jagiellonian University Medical College |
24675176 |
74 |
Solid-supported synthesis, molecular modeling, and biological activity of long-chain arylpiperazine derivatives with cyclic amino acid amide fragments as 5-HT(7) and 5-HT(1A) receptor ligands. |
Jagiellonian University Medical College |
23252794 |
56 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives ina1-adrenergic and 5-HT1A receptor binding sites recognition. |
University Of Camerino |
16730983 |
165 |
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation. |
Glaxosmithkline |
23477943 |
51 |
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression. |
Bristol-Myers Squibb |
23332346 |
69 |
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile. |
Chinese Academy Of Sciences |
23425156 |
24 |
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches. |
Novartis Pharma |
23279866 |
69 |
Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT1A/5-HT2A/5-HT7 and dopamine D2/D3 receptors. |
Jagiellonian University Medical College |
18162395 |
89 |
Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor. |
Novartis Institutes For Biomedical Research |
12443779 |
44 |
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties. |
Janssen-Cilag |
| 18 |
Synthesis and serotonergic activity of benzofuran and dihydrogenzofuran analogues of 5-carboxamidotryptamine. |
TBA |
24900506 |
39 |
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect. |
TBA |
22370341 |
29 |
Favourable involvement ofa2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement. |
University Of Camerino |
22145629 |
68 |
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergica1- and serotonine 5-HT1A receptors. |
Universit£ |
17562349 |
66 |
A chemometric study of the 5-HT(1A) receptor affinities presented by arylpiperazine compounds. |
Universidade De S£O Paulo |
20951584 |
105 |
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3. |
Glaxosmithkline |
20801662 |
60 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study. |
Universit£ |
20605276 |
61 |
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
Universit£ |
20133028 |
88 |
Pharmacophore-based 3D QSAR studies on a series of high affinity 5-HT1A receptor ligands. |
Universidade Federal Da Para£Ba |
20185311 |
72 |
Discovery of a new series of 5-HT1A receptor agonists. |
Universit£ |
19846239 |
24 |
Application of desirability-based multi(bi)-objective optimization in the design of selective arylpiperazine derivates for the 5-HT1A serotonin receptor. |
University Of Porto |
19071020 |
66 |
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II. |
Glaxosmithkline |
19286377 |
101 |
8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II. |
Glaxosmithkline |
18799312 |
84 |
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
18817363 |
84 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
Universit£ |
18829312 |
64 |
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity. |
Glaxosmithkline |
18433113 |
124 |
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
Glaxosmithkline |
16039851 |
57 |
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands. |
Glaxosmithkline |
9548813 |
53 |
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. |
Smithkline Beecham Pharmaceuticals |
9191957 |
210 |
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines. |
Universit£ |
8642566 |
277 |
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines. |
Universit£ |
7752204 |
98 |
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors. |
Merck Sharp & Dohme Research Laboratories |
8496922 |
92 |
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors. |
Merck Sharp And Dohme Research Laboratories |
11755365 |
113 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2. |
Janssen-Cilag |
11755364 |
104 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1. |
Janssen-Cilag |
11229746 |
6 |
First tricyclic oximino derivatives as 5-HT3 ligands. |
Universit£ |
11140733 |
92 |
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134). |
Smithkline Beecham Pharmaceuticals |
| 68 |
The discovery of a series of new non-indole 5HT1D agonists |
TBA |
23043306 |
69 |
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach. |
Neurosearch Sweden |
22795332 |
66 |
Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012. |
F. Hoffmann-La Roche |
21486038 |
177 |
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. |
H. Lundbeck |
23102207 |
122 |
Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers. |
Universit£ |
23006002 |
35 |
Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists. |
Suven Life Sciences |
22533875 |
11 |
Mitigating heterocycle metabolism in drug discovery. |
Amgen |
22845053 |
100 |
Structure-functional selectivity relationship studies ofß-arrestin-biased dopamine D2 receptor agonists. |
University Of North Carolina At Chapel Hill |
22738628 |
38 |
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors. |
University Of Li£Ge |
22738316 |
35 |
Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo. |
Universit£ |
22694093 |
16 |
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. |
National Institute Of Biological Sciences |
22926225 |
200 |
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT7 receptor antagonists. |
TBA |
24900202 |
38 |
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists. |
TBA |
22748706 |
52 |
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D1 receptor. |
Shenyang Pharmaceutical University |
22520153 |
135 |
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants. |
Florida A&M University |
22607670 |
34 |
Interactions of N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-2-aryl-2-yl-acetamides and 1-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-3-aryl-2-yl-ureas with dopamine D2 and 5-hydroxytryptamine 5HT(1A) receptors. |
University Of Belgrade |
22542010 |
31 |
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition. |
Amgen |
22313242 |
146 |
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists. |
Pfizer |
22313227 |
78 |
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype. |
National Institute Of Mental Health |
22268448 |
34 |
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. |
University Of Li£Ge |
21859078 |
62 |
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with highs1 receptor affinity. |
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster |
21726069 |
98 |
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
University Of Namur |
21207959 |
69 |
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging. |
National Institute Of Mental Health |
20931963 |
112 |
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome. |
Aska Pharmaceutical |
20684563 |
176 |
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. |
H. Lundbeck |
20041669 |
85 |
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist. |
Chinese Academy Of Sciences |
20153652 |
49 |
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
Universidade Federal Do Rio Grande Do Sul |
19754201 |
2 |
Physical binding pocket induction for affinity prediction. |
University Of California |
19705871 |
14 |
Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure. |
Universita Degli Studi Di Bari |
19559623 |
33 |
'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity. |
Chinese Academy Of Sciences |
19331412 |
122 |
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists. |
National Institute On Drug Abuse-Intramural Research Program |
19159187 |
38 |
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists. |
Universitat De Barcelona |
18834188 |
232 |
Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2. |
Wyeth Research |
16562853 |
22 |
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro. |
Tom'S Of Maine |
18468904 |
48 |
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand. |
Purdue University |
18083580 |
118 |
Novel quinazolinone derivatives as 5-HT7 receptor ligands. |
Institute Of Science And Technology |
18221879 |
13 |
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure. |
Westf£Lische Wilhelms-Universit£T M£Nster |
18269229 |
16 |
N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands. |
Universita Degli Studi Di Bari |
17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
18029187 |
20 |
Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors. |
University Of Missouri-Columbia |
18023344 |
77 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. |
F. Hoffmann-La Roche |
17998160 |
101 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. |
F. Hoffmann-La Roche |
18181565 |
71 |
Multi-target-directed ligands to combat neurodegenerative diseases. |
University Of Bologna |
16854086 |
96 |
Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity. |
Wyeth Research |
16789750 |
155 |
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
Laboratoire De Chimie Th�Rapeutique |
16480278 |
279 |
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
Organix |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
15658848 |
103 |
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. |
Wyeth Research |
15916420 |
68 |
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. |
Friedrich-Alexander University |
15887953 |
16 |
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan. |
Wyeth Research |
15634021 |
113 |
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands. |
Universit£ |
15357957 |
29 |
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers. |
Brigham & Women'S Hospital |
15239663 |
60 |
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction. |
Abbott Laboratories |
12519065 |
243 |
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
H. Lundbeck |
12954071 |
109 |
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. |
Alcon Research |
12825922 |
207 |
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
Virginia Commonwealth University |
12361386 |
113 |
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. |
Friedrich-Alexander University |
12213075 |
70 |
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD). |
Purdue University |
11170639 |
73 |
Current and novel approaches to the drug treatment of schizophrenia. |
Merck Sharp And Dohme Research Laboratories |
11708905 |
20 |
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy. |
Eli Lilly |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities Of Lille |
10602703 |
73 |
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent. |
Warner-Lambert |
9083484 |
84 |
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
Cooperation Pharmaceutique Fran�Aise |
8568804 |
42 |
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. |
Universit£ |
7562938 |
17 |
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists. |
Wyeth-Ayerst Research |
7658447 |
72 |
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors. |
Centre De Recherche Pierre Fabre |
7608898 |
4 |
The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site. |
Sandoz Pharma |
8097538 |
69 |
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
Upjohn Laboratories |
8101876 |
28 |
Novel 2-substituted tetrahydro-3H-benz[e]indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants. |
Upjohn Laboratories |
8496900 |
136 |
Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands. |
Upjohn Laboratories |
1348089 |
71 |
Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds. |
Upjohn Laboratories |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
11844688 |
102 |
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
Friedrich-Alexander University |
12113813 |
53 |
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
Friedrich-Alexander University |
11549463 |
72 |
Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
Friedrich-Alexander University |
10576696 |
32 |
Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands. |
Merck |
| 25 |
Pyrazolo[1,5-a]pyridines and pyrazolo[1,5-b]pyridazines as 5ht3-antagonists |
TBA |
22336245 |
72 |
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol. |
Florida A&M University |
22309909 |
37 |
Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors. |
National Medicines Institute |
22245230 |
128 |
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. |
Florida A&M University |
22029386 |
156 |
New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage. |
Universidad Complutense De Madrid |
22000209 |
54 |
Design, synthesis and in vitro evaluation of bridgehead fluoromethyl analogs of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) for the 5-HT(1A) receptor. |
Vu University Medical Center |
21866910 |
66 |
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features. |
Abbott Healthcare Products |
21782428 |
61 |
Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder. |
Lundbeck Research Usa |
21907583 |
48 |
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
University Of South Florida |
21899931 |
27 |
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands. |
The University Of Mississippi |
21823597 |
373 |
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter. |
Green Cross |
21783363 |
10 |
Synthesis and in vitro evaluation of derivatives of theß¿?-adrenergic receptor antagonist HX-CH 44. |
University Of Toronto |
21732626 |
60 |
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors. |
Washington University |
21591752 |
41 |
Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile. |
Soochow University College Of Pharmaceutical Sciences |
24900203 |
13 |
Development of Fluorescent Ligands for the Human 5-HT1A Receptor. |
TBA |
21520940 |
40 |
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor. |
Vu University Medical Center |
21495689 |
134 |
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity. |
National Institute On Drug Abuse-Intramural Research Program |
21353774 |
81 |
Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder. |
Pfizer |
21334902 |
46 |
Further SAR study on 11-O-substituted aporphine analogues: identification of highly potent dopamine D3 receptor ligands. |
Chinese Academy Of Sciences |
21093272 |
126 |
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists. |
Wyeth Research |
21190848 |
61 |
1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands. |
Korea Research Institute Of Chemical Technology |
21185183 |
111 |
Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT(1A) partial agonists. |
Pfizer |
20949929 |
63 |
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors. |
Bristol-Myers Squibb |
20932009 |
127 |
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. |
Wyeth Research |
20888762 |
7 |
Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors. |
Università |
20860381 |
61 |
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
Friedrich-Alexander University |
20812727 |
157 |
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography. |
National Institute Of Mental Health |
20801650 |
245 |
6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics. |
Pfizer |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical And Public Health Institute |
20656482 |
36 |
Synthesis and in vitro binding studies of piperazine-alkyl-naphthamides: impact of homology and sulphonamide/carboxamide bioisosteric replacement on the affinity for 5-HT1A, alpha2A, D4.2, D3 and D2L receptors. |
University Of LièGe |
20655748 |
92 |
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents. |
Korea Research Institute Of Chemical Technology |
20662542 |
64 |
Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands. |
University Of Sydney |
20620058 |
41 |
Smoothened antagonists for hair inhibition. |
Pfizer |
20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
20384344 |
42 |
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice. |
Meiji Seika Kaisha |
20363635 |
10 |
Identification of serotonin 5-HT1A receptor partial agonists in ginger. |
Department Of Chemistry And Applied Biosciences |
20443629 |
38 |
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists. |
Pfizer |
19939513 |
21 |
8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
20346662 |
4 |
The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists. |
Polish Academy Of Sciences |
20223662 |
174 |
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists. |
Yangji Chemicals |
20149649 |
133 |
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant. |
Green Cross |
19767206 |
9 |
Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors. |
National Institute Of Mental Health |
20031410 |
84 |
Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists. |
Pfizer |
20022748 |
4 |
Molecular modeling study of 4-phenylpiperazine and 4-phenyl-1,2,3,6-tetrahydropyridine derivatives: a new step towards the design of high-affinity 5-HT1A ligands. |
University Of Li£Ge |
20170099 |
58 |
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. |
Wyeth Research |
20064720 |
44 |
Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity. |
Wyeth Research |
19954972 |
14 |
Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling. |
University Of Sydney |
19932965 |
80 |
Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT(1A) receptor and the serotonin transporter. |
Wyeth Research |
19646882 |
72 |
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. |
University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj |
19773162 |
72 |
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. |
Arena Pharmaceuticals |
19739674 |
39 |
Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists. |
Universitat De Barcelona |
19854053 |
152 |
Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists. |
Pfizer |
19783143 |
65 |
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead. |
Novartis Institutes For Biomedical Research |
19719241 |
55 |
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. |
Wyeth Research |
9182127 |
9 |
Perhydrogenation of tabersonine, ans Aspidiosperma indole alkaloid. |
UniversitÉ |
| 5 |
Two 5-HT1A Receptor-Interactive Tryptamine Derivatives from the Unripe Fruit of Evodia rutaecarpa |
TBA |
15801844 |
54 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors. |
TBA |
| 26 |
Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptor |
TBA |
| 45 |
Arylpiperazide derivatives of phenylpiperazines as a new class of potent and selective 5-HT1B receptor antagonists |
TBA |
| 40 |
(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists |
TBA |
| 44 |
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists |
TBA |
| 12 |
5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonist |
TBA |
| 25 |
Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic properties |
TBA |
| 16 |
4-Aminomethyl chromans: dependence of serotonin and dopamine binding upon aromatic ring substitution |
TBA |
19329329 |
183 |
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET. |
Institute Of Nuclear Chemistry Johannes Gutenberg-University Mainz |
19326916 |
43 |
Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. |
Universidad Complutense De Madrid |
19155177 |
52 |
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. |
Florida A&M University |
19147349 |
35 |
Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists. |
Pfizer |
19053888 |
114 |
2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. |
Universita Degli Studi Di Bari |
18800769 |
80 |
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. |
Università |
18774793 |
85 |
Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol. |
National Institute On Drug Abuses |
18640038 |
74 |
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. |
Amgen |
18602261 |
65 |
Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists. |
Korea Research Institute Of Chemical Technology |
18595716 |
142 |
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
Florida A&M University |
18573659 |
47 |
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides. |
Glaxosmithkline |
18571421 |
78 |
Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives. |
Wyeth Research |
18511284 |
64 |
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor. |
Wyeth Research |
18507369 |
85 |
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide. |
Theravance |
18456500 |
56 |
Preparation of piperazine derivatives as 5-HT7 receptor antagonists. |
Ewha Womans University |
17067154 |
27 |
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. |
Uppsala University |
18160289 |
119 |
1-Aminoindanes as novel motif with potential atypical antipsychotic properties. |
Pfizer |
18053713 |
78 |
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. |
Korea Research Institute Of Chemical Technology |
18032038 |
38 |
Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives. |
Ucb Pharma |
17976986 |
80 |
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
Pfizer |
17804228 |
44 |
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. |
Eli Lilly |
17672446 |
149 |
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents. |
National Institute On Drug Abuse-Intramural Research Program |
17571866 |
49 |
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography. |
National Institute Of Mental Health |
17524641 |
69 |
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists. |
Glaxosmithkline |
17434731 |
51 |
Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors. |
Eli Lilly |
17407811 |
34 |
Novel pyridyl-fused 3-amino chroman derivatives with dual action at serotonin transporter and 5-HT1A receptor. |
Wyeth Research |
17266201 |
13 |
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands. |
Friedrich-Alexander University |
17064079 |
22 |
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. |
Università |
16759104 |
46 |
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists. |
Friedrich-Alexander University |
16722631 |
87 |
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
Predix Pharmaceuticals |
16677812 |
26 |
Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands. |
University Of Montpellier |
16621538 |
35 |
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol. |
Florida A&M University |
16563764 |
100 |
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
Friedrich-Alexander University |
16458504 |
37 |
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand. |
Columbia University College Of Physicians And Surgeons |
16392816 |
113 |
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. |
Alcon Research |
16392798 |
46 |
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. |
Columbia University College Of Physicians And Surgeons |
16361098 |
70 |
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists. |
F. Hoffmann-La Roche |
16332439 |
58 |
Studies toward the discovery of the next generation of antidepressants. Part 5: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity. |
Wyeth Research |
16298130 |
32 |
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5. |
Eli Lilly |
16219465 |
82 |
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs. |
Abbott |
16216506 |
31 |
3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective alpha(1)-adrenoceptor ligands. |
Università |
16143528 |
213 |
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. |
Columbia University College Of Physicians And Surgeons |
16139501 |
54 |
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents. |
University Of Erlangen-Nuremberg |
15828846 |
47 |
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists. |
Lundbeck Research Usa |
15771448 |
187 |
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity. |
Janssen-Cilag |
15686885 |
28 |
Studies towards the next generation of antidepressants. Part 4: derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor. |
Wyeth Research |
15603958 |
77 |
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists. |
Wyeth Research |
15546719 |
38 |
Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists. |
Eli Lilly |
15454211 |
19 |
Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity. |
Wyeth Research |
15267230 |
50 |
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists. |
Uppsala University |
15239661 |
120 |
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
Wyeth Research |
15225707 |
42 |
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype. |
University Of Erlangen-Nuremberg |
15109671 |
29 |
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4. |
Eli Lilly |
15055991 |
265 |
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor. |
Recordati |
15026055 |
22 |
The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands. |
Arqule |
14741267 |
43 |
Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands. |
Merck Sharp & Dohme Research Laboratories |
14698193 |
43 |
Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane. |
Wyeth Research |
14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
14611858 |
65 |
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands. |
Neurogen |
14592479 |
60 |
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 3. |
Eli Lilly |
12904082 |
20 |
New potential uroselective NO-donor alpha1-antagonists. |
Università |
12877591 |
36 |
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands. |
Purdue University |
12825944 |
184 |
Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides. |
Eli Lilly |
12824042 |
64 |
Advances Toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT(1A) receptor antagonism/SSRI activities. Part 2. |
Eli Lilly |
12749894 |
48 |
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1. |
Eli Lilly |
12161137 |
39 |
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
Friedrich-Alexander University |
12109911 |
47 |
Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine. |
University Center For Pharmacy |
11814784 |
53 |
Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors. |
Wyeth-Ayerst Research Laboratories |
11728188 |
53 |
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
Università |
11689074 |
112 |
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands. |
Merck Sharp & Dohme Research Laboratories |
11527728 |
56 |
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities. |
Solvay Pharma |
11448222 |
80 |
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
Istituto Chimico Farmaceutico E Tossicologico |
11378358 |
254 |
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. |
Columbia University College Of Physicians And Surgeons |
11354362 |
18 |
Conformational analysis of tandospirone in aqueous solution: lead evolution of potent dopamine D4 receptor ligands. |
Sumitomo Pharmaceuticals |
11327592 |
9 |
1,2,5-Thiadiazole derivatives are potent and selective ligands at human 5-HT1A receptors. |
Wyeth-Ayerst Research |
11311055 |
42 |
Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists. |
Uppsala University |
11277522 |
7 |
A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties. |
Purdue University |
11212112 |
24 |
Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives. |
Uppsala University |
11101361 |
37 |
Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
Purdue University |
11055342 |
21 |
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. |
Virginia Commonwealth University |
10841797 |
110 |
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists. |
The R. W. Johnson Pharmaceutical Research Institute |
10753471 |
64 |
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors. |
Uppsala University |
10715164 |
57 |
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
Virginia Commonwealth University |
10585208 |
212 |
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. |
Merck Sharp & Dohme Research Laboratories |
10498210 |
27 |
A new class of selective and potent inhibitors of neuronal nitric oxide synthase. |
Pfizer |
10464021 |
59 |
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. |
Knoll Pharmaceuticals |
10229627 |
11 |
Development of fluorine-18-labeled 5-HT1A antagonists. |
National Institutes Of Health |
10052975 |
129 |
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor. |
Merck Sharp And Dohme Research Laboratories |
9986723 |
29 |
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. |
Eli Lilly |
9873746 |
13 |
Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors. |
Centre De Recherche Pierre Fabre |
9871775 |
29 |
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. |
Centre De Recherche Pierre Fabre |
9871581 |
12 |
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist. |
Centre De Recherche Pierre Fabre |
9857099 |
94 |
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia. |
Synaptic Pharmaceutical |
9632349 |
38 |
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects. |
Pharmacia & Upjohn |
9622542 |
119 |
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
Institut De Chimie Pharmaceutique Albert Lespagnol |
9397179 |
40 |
5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. |
Centre De Recherche Pierre Fabre |
9357521 |
20 |
Differentiation between partial agonists and neutral 5-HT1B antagonists by chemical modulation of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562). |
Centre De Recherche Pierre Fabre |
9057850 |
27 |
Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites. |
Pharmacia & Upjohn |
9022796 |
57 |
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines. |
Solvay Pharma |
9016321 |
30 |
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors. |
Neurogen |
8960551 |
74 |
Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists. |
Centre De Recherche Pierre Fabre |
8941384 |
51 |
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. |
University Of Groningen |
8568822 |
80 |
Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors. |
Virginia Commonwealth University |
8459396 |
37 |
Centrally acting serotonergic agents. Synthesis and structure-activity relationships of C-1- or C-3-substituted derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin. |
Upjohn Laboratories |
8340922 |
7 |
Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
Upjohn Laboratories |
8097537 |
91 |
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives. |
Upjohn Laboratories |
8071931 |
20 |
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. |
Medical College Of Virginia/Virginia Commonwealth University |
7731016 |
55 |
Quantitative binding site model generation: compass applied to multiple chemotypes targeting the 5-HT1A receptor. |
Arris Pharmaceutical |
7658443 |
5 |
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties. |
Wellcome Research Laboratories |
2918500 |
23 |
Preparation and biodistribution of 1-[2-(3-[125I]iodo-4-aminophenyl)ethyl]-4-[3-(trifluoromethyl) phenyl]piperazine and 1-[2-(3-[125I]iodo-4-azidophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl] piperazine. |
University Of Pennsylvania |
1447752 |
28 |
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin. |
Pfizer |
1323682 |
61 |
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor. |
Upjohn |
27049670 |
47 |
Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1. |
Max Planck Institute Of Molecular Physiology |
27136302 |
52 |
Selectivity of Pyridone- and Diphenyl Ether-Based Inhibitors for the Yersinia pestis FabV Enoyl-ACP Reductase. |
University Of Wurzburg |
26943478 |
16 |
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives. |
Chulabhorn Research Institute |
26518975 |
9 |
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues. |
Peking University |
26851737 |
36 |
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies. |
University Of Karachi |
25384256 |
76 |
Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes. |
Vanderbilt University |
25797804 |
18 |
An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors. |
Kyushu Institute Of Technology |
25462626 |
6 |
Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes. |
Comsats Institute Of Information Technology |
9647472 |
5 |
Pharmacological characterization of the human melatonin Mel1a receptor following stable transfection into NIH3T3 cells. |
Universit&Aagrove |
9626023 |
49 |
Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs. |
Dallas Department Of Veterans Affairs Medical Center |
9618903 |
37 |
Melatonin receptor pharmacology: toward subtype specificity. |
King'S College London |
8887981 |
72 |
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand. |
Abbott Laboratories |
8386236 |
11 |
In vitro and in vivo pharmacological characterization of N6-cyclopentyl-9-methyladenine (N-0840): a selective, orally active A1 adenosine receptor antagonist. |
Whitby Research |
7518514 |
46 |
(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization. |
Abbott Laboratories |
2904784 |
109 |
Neuroleptic binding to human brain receptors: relation to clinical effects. |
Mayo Clinic |
1836757 |
5 |
Molecular cloning and characterization of a rat brain cDNA encoding a 5-hydroxytryptamine1B receptor. |
University Of Heidelberg |