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 |
28244748 |
119 |
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
Virginia Commonwealth University |
8258822 |
102 |
Three-dimensional quantitative structure-activity relationships of 5-HT receptor binding data for tetrahydropyridinylindole derivatives: a comparison of the Hansch and CoMFA methods. |
University of Georgia |
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 |
1992127 |
6 |
2,3-Dihydrobenzofuran analogues of hallucinogenic phenethylamines. |
Purdue University |
2342076 |
34 |
Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzenes. |
Mitsubishi Kasei |
2308135 |
28 |
A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors. |
Virginia Commonwealth University |
2457705 |
14 |
6-substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists. |
Eli Lilly |
2456389 |
40 |
Ergolines as selective 5-HT1 agonists. |
Eli Lilly |
3385733 |
28 |
Synthesis and serotonin receptor affinities of a series of enantiomers of alpha-methyltryptamines: evidence for the binding conformation of tryptamines at serotonin 5-HT1B receptors. |
Purdue University |
3572981 |
12 |
N-methyl derivatives of the 5-HT2 agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane. |
TBA |
3701781 |
14 |
Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. |
TBA |
3950904 |
26 |
5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. |
TBA |
3783602 |
22 |
2,3-Dialkyl(dimethylamino)indoles: interaction with 5HT1, 5HT2, and rat stomach fundal serotonin receptors. |
TBA |
3783595 |
14 |
5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. |
TBA |
12467617 |
17 |
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. |
Meiji Seika Kaisha |
27639363 |
141 |
Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics. |
Huazhong University of Science and Technology |
27448773 |
16 |
Steric structure-activity relationship of cyproheptadine derivatives as inhibitors of histone methyltransferase Set7/9. |
Tokyo Medical and Dental University (Tmdu) |
27061981 |
22 |
5-HT2 receptor affinity, docking studies and pharmacological evaluation of a series of 1,3-disubstituted thiourea derivatives. |
Medical University of Warsaw |
26820556 |
156 |
Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus. |
Dipartimento Di Farmacia 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 |
26483200 |
100 |
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
Huazhong University of Science and Technology |
26023814 |
79 |
Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential. |
Iqm-Csic |
25936259 |
55 |
Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent. |
Jagiellonian University Medical College |
25435254 |
82 |
Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT1A receptor functional profile. |
Jagiellonian University Medical College |
25343529 |
221 |
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
Universit£ |
24800940 |
146 |
Identification of a new selective dopamine D4 receptor ligand. |
Florida A&M University |
24618300 |
28 |
Synthesis and biological evaluation of a series of benzoxazole/benzothiazole-containing 2,3-dihydrobenzo[b][1,4]dioxine derivatives as potential antidepressants. |
Huazhong University of Science and Technology |
23353740 |
21 |
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
Universidade Federal De Goi£S |
7932524 |
38 |
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor. |
Merck Sharp & Dohme Research Laboratories |
3373482 |
50 |
Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor. |
Merrell Dow Research Institute |
| 18 |
Synthesis and serotonergic activity of benzofuran and dihydrogenzofuran analogues of 5-carboxamidotryptamine. |
TBA |
19846239 |
24 |
Application of desirability-based multi(bi)-objective optimization in the design of selective arylpiperazine derivates for the 5-HT1A serotonin receptor. |
University of Porto |
8709108 |
28 |
Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus. |
Eli Lilly |
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 |
12482418 |
18 |
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors. |
University of Santiago |
11454468 |
35 |
Discovery and SAR of org 24598-a selective glycine uptake inhibitor. |
Organon Research and Development Group |
9934473 |
16 |
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors. |
Universidad De Santiago De Compostela |
| 1 |
Synthesis, biological in vitro evaluation and stereoselectivity of ondansetron analogues: novel 5-HT2A receptor antagonists |
TBA |
22386241 |
46 |
Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents. |
Sk Biopharmaceuticals |
21816515 |
93 |
Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1. |
Medical University of Warsaw |
20931963 |
112 |
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome. |
Aska Pharmaceutical |
20153652 |
49 |
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
Universidade Federal Do Rio Grande Do Sul |
19831400 |
47 |
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization. |
European Research Centre For Drug Discovery and Development (Natsyndrugs) |
19560916 |
39 |
Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands. |
Jagiellonian University Medical College |
18603331 |
73 |
The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones. |
Jagiellonian University Medical College |
9214741 |
4 |
Activity of Parthenolide at 5HT2A receptors. |
University of Montana |
18187324 |
5 |
Total synthesis and evaluation of [18F]MHMZ. |
University of Mainz |
17517514 |
63 |
7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
Jagiellonian University Medical College |
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£ |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
15357957 |
29 |
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers. |
Brigham & Women'S Hospital |
14640559 |
405 |
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters. |
Faes Farma |
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 |
12361392 |
62 |
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors. |
Universit£ |
11784153 |
125 |
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists. |
Merck Sharp and Dohme Research Laboratories |
11784139 |
82 |
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
Universit£ |
12213075 |
70 |
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD). |
Purdue University |
11170639 |
73 |
Current and novel approaches to the drug treatment of schizophrenia. |
Merck Sharp and Dohme Research Laboratories |
10229626 |
66 |
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors. |
Universit£ |
9513601 |
53 |
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives. |
Universit£ |
9599242 |
23 |
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist. |
Astra Arcus |
9357534 |
49 |
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. |
Universit£ |
8960552 |
58 |
Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4. |
Universit£ |
7707322 |
52 |
Ketanserin analogues: the effect of structural modification on 5-HT2 serotonin receptor binding. |
Virginia Commonwealth University |
7861418 |
61 |
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
Vanderbilt University |
7629808 |
64 |
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies. |
Universit£ |
7783131 |
78 |
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. |
H. Lundbeck |
8246241 |
34 |
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography. |
University of Pennsylvania |
8410990 |
141 |
Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans. |
H. Lundbeck |
1573641 |
60 |
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype. |
Searle Research and Development |
1542100 |
67 |
Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity. |
Virginia Commonwealth University |
1346653 |
168 |
Pyrrole mannich bases as potential antipsychotic agents. |
R. W. Johnson Pharmaceutical Research Institute |
1479590 |
73 |
Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding. |
Virginia Commonwealth University |
1361578 |
99 |
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
Bristol-Myers Squibb |
1908521 |
106 |
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists. |
Centre De Recherches De Vitry Alfortville Rh£Ne-Poulenc Rorer |
1672156 |
81 |
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
Hoechst-Roussel Pharmaceuticals |
1995885 |
15 |
Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2- morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds. |
Dainippon Pharmaceutical |
1833546 |
47 |
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands. |
Abbott Laboratories |
1671416 |
15 |
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones. |
Warner-Lambert |
2258903 |
23 |
Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxa mide, a useful radioligand for 5HT3 receptors. |
Eli Lilly |
2542551 |
89 |
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
Bristol-Myers |
2903929 |
143 |
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity. |
H. Lundbeck |
3039136 |
328 |
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships. |
TBA |
2889830 |
26 |
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. |
Duphar Research Laboratories |
2888898 |
41 |
Antipsychotic activity of substituted gamma-carbolines. |
Wyeth Laboratories |
3543362 |
184 |
Central serotonin receptors as targets for drug research. |
TBA |
2874226 |
27 |
Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives. |
TBA |
2869146 |
72 |
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
TBA |
11078200 |
61 |
N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists. |
Welfide |
10843230 |
20 |
Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity. |
Yale University |
| 24 |
1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonists |
TBA |
14695828 |
107 |
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
Universit£ |
22277589 |
72 |
Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation. |
Jagiellonian University Medical College |
22133459 |
56 |
New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation. |
Universit£ |
22029386 |
156 |
New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage. |
Universidad Complutense De Madrid |
22001327 |
77 |
Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands. |
Jagiellonian University Medical College |
21440338 |
36 |
Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents. |
Universit£ |
20684606 |
68 |
Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia. |
Arena Pharmaceuticals |
20481570 |
81 |
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
Universita Di Siena |
20363131 |
4 |
Design of new dopamine D2 receptor ligands: biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581. |
Universidade Federal De Goi£S |
20347301 |
32 |
New 5-HT(1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: synthesis and in vitro pharmacological evaluation. |
Universit£ |
20060623 |
30 |
Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity. |
Jagiellonian University Medical College |
19914063 |
84 |
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. |
Pfizer |
19679379 |
33 |
Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
Jagiellonian University Medical College |
19954866 |
31 |
Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands. |
Universit£ |
15801844 |
54 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors. |
TBA |
| 52 |
Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity. |
TBA |
| 53 |
5-HT1A and 5-HT2A ligands with anxiolytic and antipanic-like properties |
TBA |
| 21 |
4-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists |
TBA |
| 43 |
2-[4-(o-methoxyphenyl)piperazin-1-ylmethyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine as a new selective 5-HT1A receptor ligand |
TBA |
| 58 |
Synthesis and serotonin receptor binding properties of 5-substituted 3-(1′,2′,5′,6′-tetrahydropyridin-3′-yl) indoles |
TBA |
| 50 |
Synthesis and evaluation of n-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives as potential anti-ischemic agents |
TBA |
19425598 |
61 |
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships. |
European Research Centre For Drug Discovery and Development (Natsyndrugs) |
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 |
19072656 |
110 |
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
University of Siena |
18598015 |
53 |
Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands. |
Università |
18467103 |
18 |
'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines. |
University of Wisconsin-La Crosse |
18296055 |
26 |
The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands. |
Purdue University |
17976986 |
80 |
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
Pfizer |
17900912 |
15 |
1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems. |
Università |
17543523 |
17 |
R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands. |
Harvard Medical School |
17419053 |
49 |
Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity. |
Alcon Research |
17328523 |
36 |
Novel sigma receptor ligands: synthesis and biological profile. |
University of Catania |
17321139 |
48 |
Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation. |
University of Montpellier |
17254782 |
28 |
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors. |
Faculté |
17251022 |
48 |
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors. |
Université |
17234413 |
4 |
Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines. |
Central Drug Research Institute |
16971119 |
35 |
Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands. |
Merck Sharp and Dohme Research Laboratories |
16970404 |
22 |
1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists. |
Purdue University |
16821786 |
13 |
C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor. |
Purdue 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 |
16107148 |
44 |
New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation. |
Università |
16061378 |
87 |
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. |
Organix |
15993598 |
55 |
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia. |
Merck Sharp and Dohme Research Laboratories |
15771414 |
36 |
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
Università |
15588097 |
95 |
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents. |
Università |
15537358 |
26 |
Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane. |
Virginia Commonwealth University |
15341484 |
159 |
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors. |
Merck |
15115407 |
8 |
New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation. |
Collegium Medicum of The Jagiellonian University |
15013010 |
9 |
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands. |
Virginia Commonwealth University |
15013009 |
28 |
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation. |
Virginia Commonwealth University |
14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
12930153 |
128 |
Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors. |
Virginia Commonwealth University |
12877591 |
36 |
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands. |
Purdue University |
12852967 |
15 |
Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor. |
Virginia Commonwealth University |
12668005 |
21 |
Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist. |
Universidad Complutense |
12570387 |
60 |
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands. |
Università |
12482441 |
45 |
Development of a presynaptic 5-HT1A antagonist. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12408724 |
79 |
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
University of LièGe |
12113827 |
7 |
Translocation of the 5-alkoxy substituent of 2,5-dialkoxyarylalkylamines to the 6-position: effects on 5-HT(2A/2C) receptor affinity. |
Purdue University |
12109911 |
47 |
Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine. |
University Center For Pharmacy |
11934576 |
85 |
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands. |
Université |
11755343 |
54 |
Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
11689074 |
112 |
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands. |
Merck Sharp & Dohme Research Laboratories |
11563927 |
75 |
1-[2-methoxy-5-(3-phenylpropyl)]-2-aminopropane unexpectedly shows 5-HT(2A) serotonin receptor affinity and antagonist character. |
Virginia Commonwealth University |
32247749 |
119 |
Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs. |
Cracow University of Technology |
11462981 |
184 |
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
Universidad De Navarra |
11354383 |
24 |
Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity. |
Polish Academy of Sciences |
11300881 |
45 |
Enantiospecific synthesis and pharmacological evaluation of a series of super-potent, conformationally restricted 5-HT(2A/2C) receptor agonists. |
Purdue University |
11277522 |
7 |
A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties. |
Purdue University |
11229772 |
16 |
Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor. |
Virginia Commonwealth University |
11101361 |
37 |
Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
Purdue University |
11055342 |
21 |
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. |
Virginia Commonwealth University |
30685525 |
34 |
Benzimidazolone-based selective ? |
University of Florida |
10956215 |
52 |
1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists. |
Virginia Commonwealth University |
10956192 |
31 |
Synthesis of novel 5-substituted 3-amino-3,4-dihydro-2H-1-benzopyran derivatives and their interactions with the 5-HT1A receptor. |
Astrazeneca R&D SöDertäLje |
10821703 |
8 |
Application of similarity matrices and genetic neural networks in quantitative structure-activity relationships of 2- or 4-(4-Methylpiperazino)pyrimidines: 5-HT(2A) receptor antagonists. |
Jagiellonian University |
10743959 |
48 |
N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. |
Yoshitomi Pharmaceutical Industries |
10715164 |
57 |
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
Virginia Commonwealth University |
10514296 |
8 |
Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain. |
Purdue 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 |
10377229 |
107 |
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
University of GöTeborg |
31253535 |
115 |
Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants. |
Cracow University of Technology |
10360740 |
35 |
N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor. |
Postech |
9986714 |
105 |
Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha1-adrenoceptor antagonists. |
Recordati |
9986703 |
7 |
Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT2A and alpha1 receptor binding affinity. |
Angelini Ricerche |
9876110 |
58 |
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
Centro De InvestigacióN Grupo Ferrer |
9873609 |
15 |
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists. |
Neurogen |
31537425 |
11 |
Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system. |
Jagiellonian University Medical College |
9871719 |
144 |
Serotonergic ergoline derivatives. |
Pharmacia & Upjohn |
9871525 |
56 |
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors. |
R. W. Johnson Pharmaceutical Research Institute |
9857084 |
11 |
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor. |
Purdue University |
9836624 |
64 |
Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding. |
Virginia Commonwealth University |
9622555 |
25 |
Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity. |
Purdue University |
9406603 |
49 |
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
University of Groningen |
9301661 |
32 |
Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives. |
Purdue University |
9276014 |
62 |
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents. |
Warner-Lambert |
9046348 |
45 |
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands. |
Università |
8893838 |
106 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. |
Universidad Complutense |
8809161 |
90 |
Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole. |
H. Lundbeck |
31547945 |
88 |
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives. |
Cracow University of Technology |
8709129 |
18 |
Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups. |
Purdue University |
8709107 |
99 |
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
Yamanouchi Pharmaceutical |
8568801 |
13 |
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
Pfizer |
8558529 |
195 |
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
Hoechst-Roussel Pharmaceuticals |
8496920 |
14 |
(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. |
Wyeth Research (Uk) |
8355253 |
74 |
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist. |
Virginia Commonwealth University |
8246239 |
84 |
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives. |
Solvay Duphar |
24211020 |
35 |
Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands. |
University of Maryland |
8101877 |
80 |
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
University of LièGe |
8064797 |
118 |
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
Vanderbilt University |
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 |
7914536 |
96 |
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
Hoechst-Roussel Pharmaceuticals |
7901415 |
36 |
Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics. |
Scios Nova |
7699712 |
20 |
Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes. |
Purdue University |
7473566 |
152 |
Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
H. Lundbeck |
6581313 |
2 |
Synthesis and evaluation of a novel series of N,N-dimethylisotryptamines. |
TBA |
17870534 |
21 |
Two new phenylpiperazines with atypical antipsychotic potential. |
Institute For Biological Research |
17869521 |
15 |
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent. |
Central Drug Research Institute |
17579386 |
7 |
Multistructure 3D-QSAR studies on a series of conformationally constrained butyrophenones docked into a new homology model of the 5-HT2A receptor. |
Universitat Pompeu Fabra |
17300168 |
81 |
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
Pierre Fabre Research Center |
12014957 |
86 |
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor. |
Meiji Seika Kaisha |
10966742 |
28 |
GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors. |
University of Perugia |
10052959 |
20 |
Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor. |
Meiji Seika Kaisha |
10514291 |
51 |
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
University of Bologna |
10425105 |
51 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
University of Camerino |
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 |
9046349 |
87 |
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. |
Faes |
9240350 |
9 |
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists. |
Monash University |
7658446 |
4 |
Effect of a chiral 4-alkyl substituent in hallucinogenic amphetamines. |
Purdue University |
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 |
7914540 |
16 |
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone. |
University of Santiago De Compostela |
30383372 |
190 |
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
Huazhong University of Science and Technology |
3746815 |
15 |
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin. |
TBA |
2965244 |
32 |
N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
Virginia Commonwealth University |
2902227 |
10 |
Serotonergic properties of spiroxatrine enantiomers. |
University of Arizona |
2902226 |
39 |
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2. |
Duphar Research Laboratories |
2892936 |
21 |
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. |
Warner-Lambert |
2875184 |
57 |
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
TBA |
28943244 |
136 |
New 5-HT |
Dipartimento Di Farmacia Universit£ |
2565400 |
132 |
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. |
Mcneil Pharmaceutical and Janssen Research Foundation Worldwide |
2537429 |
61 |
2H-[1]benzopyrano[3,4-b]pyridines: synthesis and activity at central monoamine receptors. |
Ciba-Geigy |
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 |
2299641 |
24 |
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin. |
Virginia Commonwealth University |
2213830 |
30 |
Binding of indolylalkylamines at 5-HT2 serotonin receptors: examination of a hydrophobic binding region. |
Virginia Commonwealth University |
1683407 |
32 |
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
1676758 |
12 |
Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
H. Lundbeck |
1652026 |
43 |
Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity. |
Virginia Commonwealth University |
1652023 |
179 |
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor. |
Abbott Laboratories |
1534585 |
8 |
Benzofuran bioisosteres of hallucinogenic tryptamines. |
Purdue University |
1531364 |
42 |
Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors. |
University of Pennsylvania |
1447752 |
28 |
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin. |
Pfizer |
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 |
1353116 |
10 |
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
Hoechst-Roussel Pharmaceuticals |
1348090 |
64 |
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. |
H. Lundbeck |
1336054 |
63 |
Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles. |
H. Lundbeck |
1336053 |
86 |
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles. |
H. Lundbeck |
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 |
26218629 |
26 |
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1). |
Oregon Health & Science University |
26214585 |
23 |
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents. |
University of Wisconsin-Madison |
26119990 |
19 |
Synthesis, biological evaluation and molecular docking of N-phenyl thiosemicarbazones as urease inhibitors. |
University of Karachi |
25462625 |
58 |
Salicylanilide diethyl phosphates as cholinesterases inhibitors. |
Charles University In Prague |
10747922 |
12 |
Compulsory order of substrate binding to herpes simplex virus type 1 thymidine kinase. A calorimetric study. |
Swiss Federal Institute of Technology |