The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
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 |
28244748 |
119 |
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
Virginia Commonwealth University |
28274674 |
93 |
Design, synthesis and in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors. |
Chonnam National University |
28089699 |
63 |
Investigation of piperazine benzamides as humanß |
Merck |
28041833 |
52 |
X-ray structure based evaluation of analogs of citalopram: Compounds with increased affinity and selectivity compared with R-citalopram for the allosteric site (S2) on hSERT. |
3D-2Drug |
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 |
27939174 |
84 |
Challenges in the development of an M |
Vanderbilt University Medical Center |
27865645 |
62 |
Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HT |
Sumitomo Dainippon Pharma |
27537923 |
31 |
Novel bis-arylalkylamines as myeloperoxidase inhibitors: Design, synthesis, and structure-activity relationship study. |
Universit£ |
27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University Of Kansas |
27280968 |
6 |
Polycyclic Polyprenylated Acylphloroglucinol Congeners from Hypericum scabrum. |
Chinese Academy Of Medical Sciences And Peking Union Medical College |
27364609 |
230 |
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. |
Florida A&M University |
27325446 |
42 |
Design, synthesis, and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitors - Part 3. |
Takeda Pharmaceutical |
27312422 |
219 |
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands. |
Florida A&M University |
27160055 |
76 |
Synthesis and inhibitory evaluation of 3-linked imipramines for the exploration of the S2 site of the human serotonin transporter. |
Aarhus University |
27041397 |
24 |
Design, synthesis, and biological evaluation of arylpiperazine-benzylpiperidines with dual serotonin and norepinephrine reuptake inhibitory activities. |
Chonnam National University |
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 |
26935940 |
23 |
Emerging targets and new small molecule therapies in Parkinson's disease treatment. |
School Of Medicine Of University Of Electronic Science And Technology Of China |
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 |
26709102 |
142 |
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. |
Merck Research Laboratories |
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 |
26372073 |
1 |
Reengineered tricyclic anti-cancer agents. |
Icahn School Of Medicine At Mt. Sinai |
26337019 |
22 |
Design and synthesis of 4-benzylpiperidine carboxamides as dual serotonin and norepinephrine reuptake inhibitors. |
Chonnam National University |
26233799 |
15 |
Ethylenedioxy homologs of N-methyl-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) and its corresponding cathinone analog methylenedioxymethcathinone: Interactions with transporters for serotonin, dopamine, and norepinephrine. |
Virginia Commonwealth University |
25164761 |
41 |
Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors. |
Shanghai Institute Of Pharmaceutical Industry |
26051602 |
51 |
Design, synthesis and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitor. |
Takeda Pharmaceutical |
26153715 |
4 |
Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram. |
National Institute On Drug Abuse |
25695425 |
62 |
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
City University Of New York |
25557493 |
109 |
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
Jagiellonian University Collegium Medicum |
25070422 |
126 |
Further evaluation of the tropane analogs of haloperidol. |
Florida A&M University |
25050161 |
112 |
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors. |
Amri |
25017029 |
39 |
Design, synthesis, and biological activities of 1-aryl-1,4-diazepan-2-one derivatives as novel triple reuptake inhibitors. |
Takeda Pharmaceutical |
24974340 |
90 |
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors. |
Korea University |
24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
25221656 |
116 |
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-a-Oxyazetidine. |
Korea University |
24944732 |
37 |
Hybrid dopamine uptake blocker-serotonin releaser ligands: a new twist on transporter-focused therapeutics. |
Rti International |
24944746 |
13 |
Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram. |
National Institute On Drug Abuse-Intramural Research Program |
24805037 |
380 |
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. |
Adamed |
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 |
24187998 |
96 |
Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. |
University Of Copenhagen |
23581551 |
75 |
Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors. |
Universit£ |
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 |
23385211 |
6 |
Basic N-interlinked imipramines show apoptotic activity against malignant cells including Burkitt's lymphoma. |
Trinity College |
23253443 |
135 |
Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression. |
Bristol-Myers Squibb Research And Development |
23168018 |
10 |
A rhodamine-labeled citalopram analogue as a high-affinity fluorescent probe for the serotonin transporter. |
National Institute On Drug Abuse-Intramural Research Program |
24900562 |
126 |
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity. |
Astrazeneca |
23265880 |
8 |
A new single-photon emission computed tomography (SPECT) imaging agent for serotonin transporters: [(125)I]Flip-IDAM, (2-((2-((dimethylamino)methyl)-4-iodophenyl)thio)phenyl)methanol. |
University Of Pennsylvania |
23061607 |
10 |
Organosilicon molecules with medicinal applications. |
University Of California Davis |
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 |
19592243 |
66 |
Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors. |
Roche Palo Alto |
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 |
18433113 |
124 |
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
Glaxosmithkline |
15745809 |
15 |
Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12657274 |
109 |
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists. |
Abbott Laboratories |
23084899 |
102 |
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors. |
Amri |
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 |
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 |
22082561 |
9 |
Characterisation of [¹¹C]PR04.MZ in Papio anubis baboon: a selective high-affinity radioligand for quantitative imaging of the dopamine transporter. |
Johannes Gutenberg University |
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 |
21413808 |
170 |
Synopsis of some recent tactical application of bioisosteres in drug design. |
Bristol-Myers Squibb Pharmaceutical Research And Development |
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 |
22224640 |
53 |
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis. |
Oxagen |
22938049 |
29 |
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors. |
Korea Institute Of Science And Technology |
22608762 |
25 |
Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors. |
Shanghai Institute Of Pharmaceutical Industry |
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 |
22607684 |
50 |
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands. |
The University Of Sydney |
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 |
22398259 |
87 |
Synthesis and structure-activity relationship studies of 3-biaryl-8-oxabicyclo[3.2.1]octane-2-carboxylic acid methyl esters. |
Tubitak Mam Chemistry Institute P K 21 Gebze |
21927645 |
1 |
NO-SSRIs: Nitric Oxide Chimera Drugs Incorporating a Selective Serotonin Reuptake Inhibitor. |
TBA |
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 |
21058665 |
52 |
Nicotinic Acetylcholine Receptor Efficacy and Pharmacological Properties of 3-(Substituted phenyl)-2ß-substituted Tropanes. |
Research Triangle Institute |
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 |
20875743 |
90 |
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela |
Pfizer |
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 |
20724153 |
31 |
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors. |
Korea Institute Of Science And Technology |
20597489 |
17 |
Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography. |
Emory University |
20471260 |
146 |
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity. |
Pfizer |
20153188 |
44 |
Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores. |
Pfizer |
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 |
19740668 |
48 |
Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. |
Human Biomolecular Research Institute |
19720528 |
54 |
Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia. |
Wyeth Research |
19821575 |
47 |
Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues. |
Glaxosmithkline |
19523837 |
54 |
Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters. |
Research Triangle Institute |
19821577 |
178 |
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
Research Triangle Institute |
19722525 |
31 |
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors. |
Wyeth Research |
19329313 |
50 |
3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors. |
Wyeth Research |
17846138 |
26 |
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
Veterans Affairs Medical Center |
19201198 |
210 |
2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. |
Human Biomolecular Research Institute |
18954038 |
62 |
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain. |
Neurocrine Biosciences |
19159187 |
38 |
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists. |
Universitat De Barcelona |
18800760 |
96 |
Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists. |
Emory University |
19067522 |
18 |
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter. |
Emory University |
19014888 |
52 |
Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
Human Biomolecular Research Institute |
18951020 |
34 |
Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors. |
Wyeth Research |
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 |
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 |
18771916 |
37 |
Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors. |
Wyeth Research |
18760923 |
37 |
Synthesis and biological affinity of new imidazo- and indol-arylpiperazine derivatives: further validation of a pharmacophore model for alpha(1)-adrenoceptor antagonists. |
Universit£ |
18550369 |
82 |
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI). |
Neurocrine Biosciences |
18539031 |
126 |
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors. |
Neurocrine Biosciences |
18672364 |
119 |
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability. |
Neurocrine Biosciences |
18556210 |
75 |
Synthesis and monoamine transporter binding properties of 2beta-[3'-(substituted benzyl)isoxazol-5-yl]- and 2beta-[3'-methyl-4'-(substituted phenyl)isoxazol-5-yl]-3beta-(substituted phenyl)tropanes. |
Research Triangle Institute |
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 |
18434164 |
42 |
Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives. |
Research Triangle Institute |
18417343 |
62 |
Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity. |
Pfizer |
18313294 |
68 |
[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors. |
Pfizer |
18221879 |
13 |
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure. |
Westf£Lische Wilhelms-Universit£T M£Nster |
18053732 |
26 |
The synthesis of bivalent 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters. |
Organix |
18207394 |
126 |
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. |
Neurocrine Bioscience |
18468895 |
102 |
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors. |
Neurocrine Bioscience |
18445525 |
141 |
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors. |
Neurocrine Bioscience |
17983754 |
21 |
Synthesis, in vitro characterization, and radiolabeling of reboxetine analogs as potential PET radioligands for imaging the norepinephrine transporter. |
Emory University |
18242987 |
75 |
In vitro and in vivo evaluation of O-alkyl derivatives of tramadol. |
Sepracor |
18240382 |
104 |
1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity. |
Pfizer |
18060777 |
158 |
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
18181565 |
71 |
Multi-target-directed ligands to combat neurodegenerative diseases. |
University Of Bologna |
17766113 |
51 |
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17446076 |
187 |
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. |
University Of Aarhus |
17407815 |
27 |
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism. |
Janssen-Cilag |
16279803 |
59 |
Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes. |
Research Triangle Institute |
15566309 |
69 |
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
Research Triangle Institute |
17228864 |
328 |
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
Massachusetts College Of Pharmacy And Health Sciences |
16750359 |
58 |
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor. |
Pfizer |
16750363 |
101 |
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors. |
Pfizer |
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 |
16854064 |
65 |
Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol. |
Research Triangle Institute |
16480278 |
279 |
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
Organix |
16257206 |
18 |
Derivatives of tramadol for increased duration of effect. |
Sepracor |
16213721 |
60 |
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands. |
National Institute On Drug Abuse-Intramural Research Program |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
16162005 |
30 |
Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15828826 |
17 |
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol. |
Medical University Of South Carolina |
15546718 |
28 |
Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transporters. |
Organix |
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 |
12723940 |
145 |
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
Research Triangle Institute |
12213053 |
117 |
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
Drew University |
11472216 |
89 |
Synthesis of 6- and 7- hydroxy-8-azabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters. |
Organix |
11150168 |
165 |
Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
Pharm-Eco Laboratories |
10649976 |
72 |
Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. |
Massachusetts General Hospital |
10956207 |
43 |
2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters. |
Organix |
10821718 |
69 |
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
Georgetown University Medical Center |
10479296 |
66 |
Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. |
Massachusetts General Hospital |
9804682 |
12 |
TROTEC-1: a new high-affinity ligand for labeling of the dopamine transporter. |
Institut F£R Bioanorganische Und Radiopharmazeutische Chemie |
9276012 |
53 |
2-Carbomethoxy-3-aryl-8-oxabicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters. |
Organix |
8558504 |
43 |
2-Carbomethoxy-3-(diarylmethoxy)-1 alpha H, 5 alpha H-tropane analogs: synthesis and inhibition of binding at the dopamine transporter and comparison with piperazines of the GBR series. |
Organix |
8027983 |
16 |
The discovery of an unusually selective and novel cocaine analog: difluoropine. Synthesis and inhibition of binding at cocaine recognition sites. |
Organix |
8464040 |
21 |
Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging. |
Organix |
7452682 |
76 |
3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake. |
TBA |
12565962 |
41 |
Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors. |
University Of Michigan |
14592523 |
42 |
Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes. |
Organix |
12798324 |
36 |
Bivalent biogenic amine reuptake inhibitors. |
Human Biomolecular Research Institute |
10698458 |
26 |
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. |
Georgetown University Medical Center |
10206550 |
28 |
Bicyclo[3.2.1]octanes: synthesis and inhibition of binding at the dopamine and serotonin transporters. |
Organix |
9871604 |
114 |
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group. |
Hong Kong University Of Science And Technology |
| 8 |
Synthesis and pharmacological characterization of A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibition |
TBA |
22309909 |
37 |
Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors. |
National Medicines Institute |
22300887 |
8 |
QSAR study and synthesis of new phenyltropanes as ligands of the dopamine transporter (DAT). |
University Of Tours |
22123324 |
36 |
Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2. |
Amgen |
22037049 |
62 |
Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class. |
Research Triangle Institute |
21458259 |
29 |
Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter. |
Key Laboratory Of Radiopharmaceuticals (Beijing Normal University) |
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 |
21916421 |
68 |
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152). |
Pfizer |
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 |
21319801 |
54 |
Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine. |
Research Triangle Institute |
21398123 |
56 |
The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS). |
Astrazeneca Charnwood |
21310612 |
99 |
Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor. |
Sunovion Pharmaceuticals |
21310609 |
108 |
Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor. |
Sunovion Pharmaceuticals |
21227702 |
9 |
Synthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1-propenes as a new class of anticancer agents. |
Trinity College |
21095126 |
60 |
Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor. |
Sunovion Pharmaceuticals |
21093273 |
154 |
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors. |
Sepracor |
21146989 |
46 |
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands. |
The University Of Sydney |
21146984 |
58 |
The synthesis and biological evaluation of 2-(3-methyl or 3-phenylisoxazol-5-yl)-3-aryl-8-thiabicyclo[3.2.1]octanes. |
Organix |
21112782 |
80 |
The identification, and optimisation of hERG selectivity, of a mixed NET/SERT re-uptake inhibitor for the treatment of pain. |
Msd |
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 |
20945906 |
33 |
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain. |
Abbott Laboratories |
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 |
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 |
20692833 |
41 |
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B. |
Csiro Molecular And Health Technologies |
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 |
20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
20509659 |
182 |
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. |
Barrow Neurological Institute |
20466553 |
6 |
Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioamphetamines. |
Trinity College |
20529687 |
3 |
Synthesis and in vivo evaluation of [11C]MPTQ: a potential PET tracer for alpha2A-adrenergic receptors. |
Columbia University |
20462211 |
92 |
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231). |
Pfizer |
20378347 |
27 |
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors. |
Wyeth Research |
20347298 |
28 |
Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia. |
Wyeth Research |
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 |
19717215 |
56 |
Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents. |
Trinity College |
19647430 |
104 |
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration. |
Pfizer |
20034793 |
31 |
Synthesis and hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles. |
Bristol-Myers Squibb |
20031410 |
84 |
Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists. |
Pfizer |
19926484 |
26 |
Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands. |
University Of Tours |
20158204 |
136 |
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. |
Research Triangle Institute |
20131864 |
59 |
1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors. |
Wyeth Research |
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 |
19560930 |
69 |
An extended study of dimeric phenyl tropanes. |
Aarhus University |
19740658 |
73 |
Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. |
Pfizer |
19632110 |
29 |
Discovery of a new series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols. |
Wyeth Research |
19739674 |
39 |
Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists. |
Universitat De Barcelona |
19713106 |
66 |
Structure-activity relationships of the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ol series of monoamine reuptake inhibitors. |
Wyeth Research |
19854053 |
152 |
Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists. |
Pfizer |
19791802 |
21 |
Synthesis of 1,1-[1-naphthyloxy-2-thiophenyl]-2-methylaminomethylcyclopropanes and their evaluation as inhibitors of serotonin, norepinephrine, and dopamine transporters. |
Oregon State University |
19616432 |
176 |
Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template. |
Pfizer |
19596193 |
72 |
Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists. |
Tsukuba Research Institute |
19560923 |
20 |
Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
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 |
19359175 |
132 |
4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships. |
Pfizer |
8496700 |
16 |
The Role of Receptor Binding in Drug Discovery |
TBA |
19492813 |
56 |
Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues. |
Glaxosmithkline |
19445453 |
87 |
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. |
National Institute On Drug Abuse-Intramural Research Program |
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 |
19282174 |
85 |
Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. |
Pfizer |
19053782 |
18 |
Synthesis, radiosynthesis, and biological evaluation of fluorine-18-labeled 2beta-carbo(fluoroalkoxy)-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography. |
Emory University |
19053748 |
57 |
Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter. |
Research Triangle Institute |
18954985 |
111 |
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors. |
Roche Palo Alto |
18954981 |
108 |
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics. |
Neurocrine Biosciences |
18948001 |
179 |
Quantitative structure-activity relationship of phenoxyphenyl-methanamine compounds with 5HT2A, SERT, and hERG activities. |
Pfizer |
18783208 |
11 |
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function. |
National Institute Of Mental Health |
18782666 |
34 |
Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines. |
Pfizer |
18701276 |
97 |
Highly functionalized 7-azaindoles as selective PPAR gamma modulators. |
Merck Research Laboratories |
18667309 |
123 |
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint. |
Neurocrine Biosciences |
18644726 |
36 |
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination. |
Institut FüR InterdisziplinäRe Isotopenforschung |
18625557 |
60 |
N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors. |
Pfizer |
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 |
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 |
18571404 |
132 |
Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines. |
Pfizer |
18557608 |
108 |
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors. |
Wyeth Research |
18487050 |
36 |
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter. |
Hadassah Hebrew University Hospital |
18461921 |
65 |
Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions. |
University Of Maryland |
17698848 |
4 |
Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter. |
Yale University |
18085744 |
12 |
Synthesis and in vivo evaluation of halogenated N,N-dimethyl-2-(2'-amino-4'-hydroxymethylphenylthio)benzylamine derivatives as PET serotonin transporter ligands. |
Emory University |
18052090 |
39 |
2-(2'-((dimethylamino)methyl)-4'-(fluoroalkoxy)-phenylthio)benzenamine derivatives as serotonin transporter imaging agents. |
University Of Pennsylvania |
17900912 |
15 |
1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems. |
Università |
17869101 |
60 |
High dopamine transporter selectivity can be displayed by remarkably simple non-nitrogen containing inhibitors. |
University Of Aarhus |
17766114 |
2 |
Synthesis and characterization of a pegylated derivative of 3-(1,2,3,6-tetrahydro-pyridin-4yl)-1H-indole (IDT199): a high affinity SERT ligand for conjugation to quantum dots. |
Vanderbilt University |
17765543 |
56 |
Dual serotonin transporter inhibitor/histamine H3 antagonists: development of rigidified H3 pharmacophores. |
Johnson & Johnson Pharmaceutical Research And Development |
17761416 |
53 |
The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors. |
Merck Research Laboratories |
17705359 |
3 |
Synthesis and in vivo evaluation of fluorine-18 and iodine-123 labeled 2beta-carbo(2-fluoroethoxy)-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane as a candidate serotonin transporter imaging agent. |
Emory University |
17690258 |
2 |
LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake. |
New York University School Of Medicine |
17616397 |
107 |
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
17583504 |
51 |
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
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 |
17446069 |
15 |
Synthesis and biological evaluation of 2beta,3alpha-(substituted phenyl)nortropanes as potential norepinephrine transporter imaging agents. |
Emory University |
17434731 |
51 |
Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors. |
Eli Lilly |
17418570 |
141 |
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17412583 |
81 |
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity. |
Johnson & Johnson Pharmaceutical Research & Development |
17391962 |
27 |
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17307358 |
81 |
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
17267217 |
76 |
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors. |
Pfizer |
17154506 |
6 |
Synthesis, radiosynthesis, and biological evaluation of carbon-11 labeled 2beta-carbomethoxy-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography. |
Emory University |
17127059 |
96 |
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors. |
Johnson & Johnson Pharmaceutical Research And Development |
17107798 |
90 |
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore. |
Johnson & Johnson Pharmaceutical Research And Development |
16931001 |
93 |
2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16784855 |
22 |
Synthesis and monoamine transporter affinity of front bridged tricyclic 3beta-(4'-halo or 4'-methyl)phenyltropanes bearing methylene or carbomethoxymethylene on the bridge to the 2beta-position. |
Emory University |
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 |
16513343 |
3 |
(R)-sila-venlafaxine: a selective noradrenaline reuptake inhibitor for the treatment of emesis. |
Paradigm Therapeutics |
16509591 |
75 |
Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivity. |
Niddk |
16497500 |
128 |
N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake. |
Eli Lilly |
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 |
16451060 |
3 |
Evaluation of carbon-11-labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]nortropane as a potential radioligand for imaging the serotonin transporter by PET. |
Emory University |
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 |
16337793 |
39 |
Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands. |
University Of Tours |
16314097 |
113 |
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine. |
Pfizer |
16302792 |
19 |
Rhodamine-labeled 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)tropane analogues as high-affinity fluorescent probes for the dopamine transporter. |
National Institute On Drug Abuse-Intramural Research Program |
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 |
16202585 |
30 |
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes. |
University Of Illinois At Chicago |
16183285 |
4 |
Inhibitors of the serotonin transporter protein (SERT): the design and synthesis of biotinylated derivatives of 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indoles. High-affinity serotonergic ligands for conjugation with quantum dots. |
Vanderbilt University |
16137883 |
84 |
1-Aryl-3,4-dihydro-1H-quinolin-2-one derivatives, novel and selective norepinephrine reuptake inhibitors. |
Eli Lilly |
15974579 |
36 |
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands. |
Emory University |
15801845 |
45 |
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents. |
Columbia University College Of Physicians And Surgeons |
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 |
15456270 |
24 |
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent. |
University Of Pennsylvania |
15357973 |
24 |
Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
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 |
15177457 |
39 |
Synthesis and biological activity of some known and putative duloxetine metabolites. |
Eli Lilly |
15125959 |
72 |
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety. |
Janssen-Cilag |
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 |
15081025 |
23 |
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA). |
Virginia Commonwealth University |
15080991 |
38 |
Synthesis and monoamine transporter affinity of 3'-analogs of 2-beta-carbomethoxy-3-beta-(4'-iodophenyl)tropane (beta-CIT). |
Yale School Of Medicine |
14971892 |
32 |
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter. |
Emory University |
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 |
14643350 |
38 |
Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake. |
Eli Lilly |
14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
12951108 |
63 |
Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression. |
Eli Lilly |
12877586 |
40 |
A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain. |
Organix |
12620070 |
24 |
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography. |
Emory University |
12372513 |
102 |
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation. |
Neurogen |
12361398 |
19 |
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine). |
University Of Pennsylvania |
12213078 |
31 |
Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter. |
Niddk |
12213054 |
38 |
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
Drew University |
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 |
10956218 |
12 |
Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines. |
Centre For Addiction And Mental Health |
10715164 |
57 |
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
Virginia Commonwealth University |
10691690 |
6 |
Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography. |
Emory University |
10669578 |
44 |
New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides. |
University Of Groningen |
10576690 |
13 |
Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine. |
Georgetown University Medical Center |
9986702 |
11 |
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol. |
University Of Pennsylvania |
9871666 |
4 |
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons. |
Novartis Pharma |
9703474 |
21 |
Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter. |
Organix |
9191960 |
21 |
A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain. |
Organix |
8515428 |
2 |
Enantioselectivity of cocaine recognition sites: binding of (1S)- and (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane (beta-CIT) to monoamine transporters. |
Northeastern University |
22803662 |
7 |
Synthesis, antielastase, antioxidant and radical scavenging activities of 4-(aza substituted) methylene substituted dihydroxy coumarines. |
Giresun University |
26864917 |
3 |
Discovery of Novel Allosteric Eg5 Inhibitors Through Structure-Based Virtual Screening. |
Southern Research Institute |
26943478 |
16 |
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives. |
Chulabhorn Research Institute |
26214585 |
23 |
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents. |
University Of Wisconsin-Madison |
9349523 |
22 |
Cloning and expression of a human serotonin 5-HT4 receptor cDNA. |
Janssen Research Foundation |
2530094 |
94 |
The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. |
Novo Industri |
16807364 |
18 |
Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs. |
Queen'S University |
19326941 |
104 |
Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6. |
Washington University |
18221310 |
180 |
Rhodanine derivatives as selective protease inhibitors against bacterial toxins. |
Burnham Institute For Medical Research |
16731764 |
10 |
CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. |
Celera Genomics |
18434145 |
56 |
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. |
Methylgene |
15771455 |
110 |
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties. |
Universita Degli Studi Di Firenze |