The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28657744 |
167 |
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
University of Illinois At Chicago |
| 28635286 |
207 |
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT |
Bristol-Myers Squibb |
| 28319392 |
216 |
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 8515429 |
16 |
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor. |
Smithkline Beecham Pharmaceuticals |
| 14741248 |
79 |
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics. |
Universidad De Santiago De Compostela |
| 12467617 |
17 |
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. |
Meiji Seika Kaisha |
| 12392747 |
36 |
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties. |
Glaxosmithkline |
| 11992776 |
70 |
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists. |
Glaxosmithkline |
| 11266169 |
27 |
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor. |
Smithkline Beecham Pharmaceuticals |
| 11597412 |
116 |
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor. |
Glaxosmithkline |
| 11459658 |
18 |
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor. |
Glaxosmithkline |
| 10969987 |
63 |
1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists. |
Smithkline Beecham Pharmaceuticals |
| 10969986 |
123 |
1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents. |
Smithkline Beecham Pharmaceuticals |
| 27876250 |
60 |
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
Jagiellonian University Medical College |
| 27908761 |
55 |
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache. |
Eli Lilly |
| 27864071 |
116 |
Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT |
Arena Pharmaceuticals |
| 27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
| 27933810 |
166 |
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 27717652 |
275 |
Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors. |
Florida A&M University |
| 27364609 |
230 |
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. |
Florida A&M University |
| 27261181 |
45 |
New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands. |
City University of New York |
| 27173799 |
97 |
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics. |
Shanghai Institute of Materia Medica |
| 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 |
| 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 |
| 26820449 |
84 |
Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives. |
Universit£ |
| 26748694 |
44 |
The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands. |
Gedeon Richter |
| 26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
| 26516782 |
59 |
Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold. |
University of Copenhagen |
| 26475518 |
19 |
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor. |
City University of New York |
| 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 |
| 25583099 |
56 |
Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists. |
University of Copenhagen |
| 25695425 |
62 |
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
City University of New York |
| 25815155 |
21 |
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. |
University of Cambridge |
| 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 |
| 25422861 |
78 |
In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 25703249 |
132 |
Novel 4-substituted-N,N-dimethyltetrahydronaphthalen-2-amines: synthesis, affinity, and in silico docking studies at serotonin 5-HT2-type and histamine H1 G protein-coupled receptors. |
University of Florida |
| 25684421 |
24 |
Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists. |
Ewha Womans University |
| 25127461 |
36 |
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression. |
Yonsei University |
| 24916029 |
42 |
Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Part 2. |
Astellas Pharma |
| 24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
| 25343529 |
221 |
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
Universit£ |
| 24878269 |
50 |
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands. |
University of Copenhagen |
| 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 |
| 24704027 |
31 |
Lactam and oxazolidinone derived potent 5-hydroxytryptamine 6 receptor antagonists. |
Cephalon |
| 24900826 |
22 |
Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects. |
Therachem Research Medilab (India) |
| 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 |
| 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 |
| 23466228 |
6 |
[11C]olanzapine, radiosynthesis and lipophilicity of a new potential PET 5-HT2 and D2 receptor radioligand. |
Indiana University School of Medicine |
| 23353740 |
21 |
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
Universidade Federal De Goi£S |
| 23301527 |
97 |
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties. |
University of Copenhagen |
| 23177783 |
130 |
Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists. |
Bristol-Myers Squibb Research and Development |
| 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 |
| 20674357 |
66 |
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders. |
Glaxosmithkline |
| 19796944 |
38 |
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
Universidad De Santiago De Compostela |
| 19146417 |
70 |
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor. |
Glaxosmithkline |
| 18783204 |
49 |
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics. |
Universidad De Santiago De Compostela |
| 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 |
| 16168649 |
65 |
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists. |
Glaxosmithkline |
| 12646038 |
19 |
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist. |
F. Hoffmann-La Roche |
| 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 |
| 22959245 |
175 |
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs). |
The University of Sydney |
| 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 |
| 23641311 |
38 |
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design. |
TBA |
| 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 |
| 24900481 |
17 |
A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold. |
TBA |
| 22845053 |
100 |
Structure-functional selectivity relationship studies ofß-arrestin-biased dopamine D2 receptor agonists. |
University of North Carolina At Chapel Hill |
| 22694093 |
16 |
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. |
National Institute of Biological Sciences |
| 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 |
| 22542010 |
31 |
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition. |
Amgen |
| 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 |
| 22309223 |
70 |
Melanin-concentrating hormone receptor 1 antagonists. Synthesis and structure-activity relationships of novel 3-(aminomethyl)quinolines. |
Takeda Pharmaceutical |
| 22778800 |
24 |
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity. |
TBA |
| 22381048 |
45 |
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists. |
Monash University (Parkville Campus) |
| 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 |
| 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 |
| 20570529 |
65 |
Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes. |
University of North Texas Health Science Center |
| 19963380 |
38 |
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. |
Hunter College and The Graduate Center of The City University of New York |
| 19159187 |
38 |
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists. |
Universitat De Barcelona |
| 18847250 |
37 |
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation. |
Virginia Commonwealth University |
| 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 |
| 18361484 |
61 |
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists. |
Egis Pharmaceuticals |
| 18083580 |
118 |
Novel quinazolinone derivatives as 5-HT7 receptor ligands. |
Institute of Science and Technology |
| 18083579 |
33 |
Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. |
Astellas Pharma |
| 18035544 |
52 |
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists. |
Astellas Pharma |
| 17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
| 18023344 |
77 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. |
F. Hoffmann-La Roche |
| 18282705 |
69 |
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists. |
Johnson & Johnson Pharmaceutical Research and Development |
| 17998160 |
101 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. |
F. Hoffmann-La Roche |
| 17314044 |
100 |
2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands. |
Merck Sharp and Dohme Research Laboratories |
| 17887659 |
58 |
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity. |
Bayer Pharmaceuticals |
| 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 |
| 16250647 |
71 |
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
Universit£ |
| 15658848 |
103 |
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. |
Wyeth Research |
| 14998318 |
112 |
Selective optimization of side activities: another way for drug discovery. |
Prestwick Chemical |
| 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 |
| 11784153 |
125 |
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists. |
Merck Sharp and Dohme Research Laboratories |
| 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 |
| 9083484 |
84 |
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
Cooperation Pharmaceutique Fran�Aise |
| 1833546 |
47 |
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands. |
Abbott Laboratories |
| 3543362 |
184 |
Central serotonin receptors as targets for drug research. |
TBA |
| 15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
| 22325948 |
52 |
Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia. |
Arena Pharmaceuticals |
| 22226656 |
75 |
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test. |
Cephalon |
| 22336245 |
72 |
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol. |
Florida A&M University |
| 22301214 |
4 |
Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I). |
University of Lille |
| 22153942 |
50 |
5-HT2c receptor selectivity and structure-activity relationship of N-methyl-N-(1-methylpiperidin-4-yl)benzenesulfonamide analogs. |
Korea Institute of Science and Technology |
| 21866910 |
66 |
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features. |
Abbott Healthcare Products |
| 21907583 |
48 |
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
University of South Florida |
| 21823597 |
373 |
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter. |
Green Cross |
| 20719507 |
37 |
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands. |
University of Copenhagen |
| 21195614 |
56 |
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
Pfizer |
| 21093272 |
126 |
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists. |
Wyeth Research |
| 21146986 |
50 |
Novel 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohepta[f]indene analogues as potent and selective 5-HT(2C) agonists for the treatment of metabolic disorders. |
Evotec |
| 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 |
| 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 |
| 20933409 |
50 |
Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant. |
Green Cross |
| 20857909 |
176 |
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors. |
University of Copenhagen |
| 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 |
| 20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
| 20692833 |
41 |
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B. |
Csiro Molecular and Health Technologies |
| 20655748 |
92 |
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents. |
Korea Research Institute of Chemical Technology |
| 20684606 |
68 |
Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia. |
Arena Pharmaceuticals |
| 20637635 |
180 |
Further optimization of novel pyrrole 3-carboxamides for targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant. |
Green Cross |
| 20493697 |
37 |
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders. |
Merck Sharp & Dohme |
| 20455563 |
49 |
Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis. |
Arena Pharmaceuticals |
| 19939513 |
21 |
8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
| 20223662 |
174 |
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists. |
Yangji Chemicals |
| 20202843 |
40 |
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity. |
Pfizer |
| 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 |
| 20137933 |
218 |
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity. |
Amgen |
| 20022752 |
94 |
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents. |
Bristol-Myers Squibb |
| 20096593 |
111 |
Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT(2A) receptor antagonists. |
Ewha Womans University |
| 19914063 |
84 |
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. |
Pfizer |
| 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 |
| 19716297 |
45 |
Design and synthesis of pyridazinone-based 5-HT(2C) agonists. |
Pfizer |
| 19692241 |
36 |
Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists. |
Pfizer |
| 19665894 |
93 |
Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents. |
Arena Pharmaceuticals |
| 19646865 |
45 |
Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence. |
Pfizer |
| 19523834 |
79 |
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. |
Wyeth Research |
| 19739674 |
39 |
Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists. |
Universitat De Barcelona |
| 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 |
| 19464901 |
77 |
Identification of novel serotonin 2C receptor ligands by sequential virtual screening. |
Institute of Science and Technology |
| | 44 |
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists |
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 |
| 19284718 |
191 |
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
University of Illinois At Chicago |
| 19269173 |
81 |
7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization. |
Pfizer |
| 19155177 |
52 |
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. |
Florida A&M University |
| 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 |
| 18621528 |
133 |
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity. |
Pfizer |
| 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 |
| 18583130 |
25 |
A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands. |
Wyeth Research |
| 18573659 |
47 |
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides. |
Glaxosmithkline |
| 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 |
| 11975483 |
10 |
New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea. |
The University of Mississippi |
| 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 |
| 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 |
| 17448659 |
29 |
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists. |
Cerep |
| 17328523 |
36 |
Novel sigma receptor ligands: synthesis and biological profile. |
University of Catania |
| 17315987 |
268 |
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor. |
Pharmaceutical Research Institute |
| 17174091 |
21 |
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists. |
Procter and Gamble Pharmaceuticals |
| 17107791 |
50 |
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG. |
Procter & Gamble Pharmaceuticals |
| 16971119 |
35 |
Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands. |
Merck Sharp and Dohme Research Laboratories |
| 16870427 |
38 |
Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents. |
Procter and Gamble Pharmaceuticals |
| 16750364 |
25 |
The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist. |
Athersys |
| 16722655 |
28 |
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. |
Pfizer |
| 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 |
| 16632354 |
61 |
A new class of selective, non-basic 5-HT2A receptor antagonists. |
Merck Sharp & Dohme |
| 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 |
| 16546379 |
30 |
The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists. |
Athersys |
| 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 |
| 16257207 |
96 |
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. |
Vernalis |
| 16219465 |
82 |
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs. |
Abbott |
| 16143528 |
213 |
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. |
Columbia University College of Physicians and Surgeons |
| 16134937 |
154 |
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. |
7Tm Pharma |
| 16061378 |
87 |
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. |
Organix |
| 16055331 |
45 |
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
Carlsson Research |
| 15993598 |
55 |
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia. |
Merck Sharp and Dohme Research Laboratories |
| 15975787 |
39 |
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists. |
Vernalis Research |
| 15911276 |
55 |
Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism. |
Janssen-Cilag |
| 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 |
| 15771415 |
155 |
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
Johnson & Johnson Pharmaceutical Research & Development |
| 15713408 |
96 |
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
Arena Pharmaceuticals |
| 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 |
| 15261280 |
34 |
Diaminopyrimidine and diaminopyridine 5-HT7 ligands. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 15261279 |
27 |
Aminotriazine 5-HT7 antagonists. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 15225734 |
10 |
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists. |
Argenta Discovery |
| 15125929 |
66 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. |
Janssen-Cilag |
| 15109661 |
21 |
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor. |
Wyeth Research |
| 15081042 |
84 |
Indoline derivatives as 5-HT(2C) receptor agonists. |
Vernalis Research |
| 15081025 |
23 |
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA). |
Virginia Commonwealth University |
| 14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth 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 |
| 12824036 |
77 |
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists. |
Pharmacia |
| 12824018 |
6 |
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. |
University of Sydney |
| 12643910 |
55 |
Identification of a novel series of selective 5-HT7 receptor antagonists. |
Glaxosmithkline |
| 12639577 |
105 |
Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics. |
Bristol-Myers Squibb |
| 12502367 |
17 |
New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization. |
Université |
| 12482441 |
45 |
Development of a presynaptic 5-HT1A antagonist. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 12372510 |
28 |
Synthesis and evaluation of 5-HT(2A) and 5-HT(2C) receptor binding affinities of novel pyrimidine derivatives. |
Egis Pharmaceuticals |
| 12361399 |
17 |
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding. |
Universita Di Camerino |
| 12014970 |
42 |
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging. |
Yale University |
| 11755343 |
54 |
Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
| 11514164 |
36 |
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists. |
Glaxosmithkline |
| 32631554 |
15 |
Synthesis and biological evaluation of thioadatanserin and its dialkylated products as partial 5-HTR |
Dominican College |
| 11378358 |
254 |
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. |
Columbia University College of Physicians and Surgeons |
| 11334570 |
103 |
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists. |
Merck Sharp and Dohme Research Laboratories |
| 32122737 |
85 |
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics. |
University of Chinese Academy of Sciences |
| 31952960 |
234 |
Discovery of a lead series of potent benzodiazepine 5-HT |
Arena Pharmaceuticals |
| 32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
| 31889666 |
94 |
Evaluation of anti-depressant effects of phthalazinone-based triple-acting small molecules against 5-HT |
Korea Institute of Science and Technology |
| 11133071 |
60 |
2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor. |
Merck Sharp & Dohme Research Laboratories |
| 10987434 |
41 |
Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines. |
Wyeth-Ayerst Research |
| 27508895 |
141 |
Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment. |
National Institute On Drug Abuse-Intramural Research Program |
| 10853660 |
23 |
Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity. |
Nps Allelix |
| 27381086 |
68 |
Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines. |
Pfizer |
| 30622024 |
9 |
Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT |
Csir-Central Drug Research Institute (Csir-Cdri) |
| 10737744 |
146 |
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. |
Smithkline Beecham Pharmaceuticals |
| 31526003 |
158 |
Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine D |
National Institute On Drug Abuse-Intramural Research Program |
| 30611057 |
32 |
Identification of a novel DGK? inhibitor for XLP-1 therapy by virtual screening. |
University of Piemonte Orientale |
| 32282200 |
320 |
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
Shanghaitech University |
| 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 |
| 31021617 |
136 |
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D |
University of Pennsylvania |
| 31112891 |
30 |
Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity. |
National University of Ireland Galway |
| 10090793 |
12 |
Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine. |
Purdue University |
| 30545651 |
27 |
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT |
Harvard Medical School |
| 30605331 |
236 |
Design and in Vivo Characterization of A |
Medical College of Wisconsin |
| 31445232 |
78 |
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
University of Illinois At Chicago |
| 9857084 |
11 |
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor. |
Purdue University |
| 9836617 |
30 |
Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives. |
Purdue University |
| 31009908 |
28 |
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
Northwest University |
| 9622555 |
25 |
Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity. |
Purdue University |
| 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 |
| 9357515 |
55 |
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. |
Merck Sharp and Dohme Research Laboratories |
| 9301661 |
32 |
Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives. |
Purdue University |
| 9046348 |
45 |
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands. |
Università |
| 31586817 |
96 |
Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect. |
Medical University of Warsaw |
| 30106578 |
10 |
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts. |
TBA |
| 29620897 |
5 |
Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT |
TBA |
| 31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
| 8709129 |
18 |
Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups. |
Purdue University |
| 26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
| 25281269 |
35 |
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists. |
Astellas Pharma |
| 24491146 |
4 |
Imaging evaluation of 5HT2C agonists, [(11)C]WAY-163909 and [(11)C]vabicaserin, formed by Pictet-Spengler cyclization. |
Harvard Medical School |
| 23792350 |
53 |
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
Universidade Federal Do Rio De Janeiro |
| 23683593 |
231 |
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists. |
Bristol-Myers Squibb Research and Development |
| 21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
| 18095642 |
111 |
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. |
Arena Pharmaceuticals |
| 17588750 |
26 |
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
Universidad De Santiago De Compostela |
| 17129726 |
121 |
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
| 17880057 |
131 |
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
Solvay Pharma |
| 17079142 |
42 |
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation. |
Glaxosmithkline |
| 17074479 |
96 |
Isoindolone derivatives, a new class of 5-HT2C antagonists: synthesis and biological evaluation. |
Glaxosmithkline Medicine Research Centre |
| 16839761 |
39 |
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849. |
Glaxosmithkline |
| 15887956 |
77 |
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. |
Glaxosmithkline |
| 16002289 |
65 |
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. |
Glaxosmithkline |
| 14613313 |
34 |
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp. |
Glaxosmithkline R&D |
| 12014957 |
86 |
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor. |
Meiji Seika Kaisha |
| 11262079 |
57 |
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation. |
Glaxowellcome |
| 10425088 |
101 |
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics. |
Universidad De Santiago |
| 9572885 |
118 |
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. |
Smithkline Beecham Pharmaceuticals |
| 9276022 |
90 |
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder. |
F. Hoffmann-La Roche |
| 7837236 |
19 |
(+)-cis-4,5,7a,8,9,10,11,11a-octahydro-7H-10-methylindolo[1,7- bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity. |
Sandoz Pharma |
| 30389290 |
146 |
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity. |
Texas Tech University Health Sciences Center |
| 29324345 |
122 |
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect. |
Shanghai Institute of Materia Medica |
| 29102176 |
135 |
Synthesis and biological evaluation of new naphtho- and quinolinocyclopentane derivatives as potent melatoninergic (MT |
Univ. Lille |
| 30258529 |
34 |
5-HT |
Usona Institute |
| 30028132 |
135 |
Discovery of ?-Arrestin Biased Ligands of 5-HT |
Korea Institute of Science and Technology |
| 29767995 |
34 |
Structure-Activity Relationships and Therapeutic Potentials of 5-HT |
Universit£ |
| 28745513 |
309 |
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products. |
University of The Philippines |
| 29395980 |
84 |
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs. |
University of Chinese Academy of Sciences |
| 29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
| 2374139 |
50 |
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole. |
Pfizer |
| 28958623 |
35 |
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H |
Glaxosmithkline |
| 28807572 |
74 |
Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide. |
Taisho Pharmaceutical |
| 28774576 |
134 |
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics. |
Xinjiang Technical Institute of Physics and Chemistry |
| 28776992 |
110 |
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors. |
Northwestern University |
| 28489950 |
119 |
Return of D |
University of Nebraska Medical Center |
| 28850227 |
85 |
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry. |
St. John'S University |
| 29116785 |
1 |
A Positive Allosteric Modulator of the Serotonin 5-HT |
Universidad Complutense De Madrid |
| 1433172 |
30 |
1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors. |
Pfizer |
| 22803662 |
7 |
Synthesis, antielastase, antioxidant and radical scavenging activities of 4-(aza substituted) methylene substituted dihydroxy coumarines. |
Giresun University |
| 26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
| 26931395 |
13 |
The Synthesis of 1,3,5-triazine Derivatives and JNJ7777120 Analogues with Histamine H4 Receptor Affinity and Their Interaction with PTEN Promoter. |
Jagiellonian University Medical College |
| 27064299 |
8 |
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile. |
Broad Institute |
| 23548908 |
1 |
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis. |
University of Washington |
| 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 |
| 26451651 |
20 |
Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast a-glucosidase, acetylcholinesterase and butyrylcholinesterase. |
Gc University |
| 26077890 |
33 |
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids. |
Tehran University of Medical Sciences |
| 26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
| 26364932 |
22 |
Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity. |
University of North Carolina At Chapel Hill |
| 25506816 |
42 |
Monoamine oxidase inhibitory activity of 2-aryl-4H-chromen-4-ones. |
Birla 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 |
| 11579444 |
23 |
Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA. |
The Royal Danish School of Pharmacy |
| 9536007 |
23 |
Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach. |
University of Bonn |
| 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 |
| 18221310 |
180 |
Rhodanine derivatives as selective protease inhibitors against bacterial toxins. |
Burnham Institute For Medical Research |
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