The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 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 |
| 2153822 |
77 |
1,9-Alkano-bridged 2,3,4,5-tetrahydro-1H-3-benzazepines with affinity for the alpha 2-adrenoceptor and the 5-HT1A receptor. |
Syntex Research |
| 27639363 |
141 |
Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics. |
Huazhong University of Science and Technology |
| 26390077 |
42 |
Tactical Approaches to Interconverting GPCR Agonists and Antagonists. |
University of Minnesota |
| 26820556 |
156 |
Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus. |
Dipartimento Di Farmacia Universit£ |
| 26483200 |
100 |
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
Huazhong University of Science and Technology |
| 25076379 |
87 |
Structural manipulation on the catecholic fragment of dopamine D(1) receptor agonist 1-phenyl-N-methyl-benzazepines. |
Shanghai Institute of Materia Medica (Simm) |
| 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 |
| 25965777 |
58 |
Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity. |
Jagiellonian University Medical College |
| 25759032 |
55 |
Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT1A and 5-HT7 receptor ligands. |
Universit£ |
| 25630223 |
5 |
Target engagement in lead generation. |
Eli Lilly |
| 25461308 |
64 |
Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity. Part 4. |
Medical University of Warsaw |
| 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 |
| 24900840 |
35 |
Enhancing a CH-? Interaction to Increase the Affinity for 5-HT1A Receptors. |
University of Li£Ge |
| 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 |
| 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 |
| 17125266 |
72 |
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?). |
Universit£ |
| 11454468 |
35 |
Discovery and SAR of org 24598-a selective glycine uptake inhibitor. |
Organon Research and Development Group |
| 9873561 |
29 |
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships. |
Solvay Pharma |
| 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 |
| 23124215 |
72 |
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selectivea1B-adrenoceptor antagonist. |
Universit£ |
| 21816515 |
93 |
Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1. |
Medical University of Warsaw |
| 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 |
| 19053780 |
76 |
Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
Universita Degli Studi Di Bari |
| 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£ |
| 18361484 |
61 |
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists. |
Egis Pharmaceuticals |
| 17228858 |
236 |
Advances in development of dopaminergic aporphinoids. |
Chinese Academy of Sciences |
| 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£ |
| 15914001 |
16 |
New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects. |
Daiichi Suntory Biomedical Research |
| 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 |
| 12930145 |
77 |
Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors. |
Universit£ |
| 12477356 |
137 |
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands. |
Universit£ |
| 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£ |
| 11170629 |
35 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. Study of the 5-HT(1a)/alpha(1)-adrenergic receptor affinity by classical hansch analysis, artificial neural networks, and computational simulation of ligand recognition. |
Universidad Complutense |
| 11170628 |
37 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT(1a)/alpha(1)-adrenergic receptor affinity: synthesis of a new derivative with mixed 5-HT(1a)/d(2) antagonist properties. |
Universidad Complutense |
| 10956195 |
38 |
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907). |
University Centre For Pharmacy |
| 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£ |
| 10090790 |
131 |
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs. |
Taisho Pharmaceutical |
| 10602693 |
64 |
Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents. |
Wyeth-Ayerst Research |
| 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£ |
| 9703460 |
52 |
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists. |
National Taiwan University |
| 9622541 |
97 |
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. |
R. W. Johnson Pharmaceutical Research Institute |
| 9599242 |
23 |
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist. |
Astra Arcus |
| 9111299 |
25 |
N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor. |
Yamanouchi Pharmaceutical |
| 9083484 |
84 |
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
Cooperation Pharmaceutique Fran�Aise |
| 9435894 |
206 |
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans. |
Wyeth-Ayerst Research Laboratories |
| 9357534 |
49 |
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. |
Universit£ |
| 9171874 |
50 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. 2. Three-dimensional quantitative structure-activity relationships of hydantoin-phenylpiperazine derivatives with affinity for 5-HT1A and alpha 1 receptors. A comparison of CoMFA models. |
Universidad Complutense |
| 8691479 |
24 |
trans-2-Aryl-N,N-dipropylcyclopropylamines: synthesis and interactions with 5-HT(1A) receptors. |
Uppsala University |
| 8676355 |
90 |
Structure-activity relationships of a series of substituted benzamides: potent D2/5-HT2 antagonists and 5-HT1a agonists as neuroleptic agents. |
Glaxo Wellcome |
| 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£ |
| 8863803 |
22 |
Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives. |
Universit£ |
| 8831770 |
136 |
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
Hoechst Marion Roussel |
| 8831769 |
42 |
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors. |
Uppsala University |
| 8759642 |
53 |
1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3. |
Universit£ |
| 8568804 |
42 |
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. |
Universit£ |
| 7473548 |
74 |
N-aryl-N'-benzylpiperazines as potential antipsychotic agents. |
R. W. Johnson Pharmaceutical Research Institute |
| 7473547 |
103 |
Piperazinylalkyl heterocycles as potential antipsychotic agents. |
R. W. Johnson Pharmaceutical Research Institute |
| 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£ |
| 7783153 |
189 |
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 2. Effects of 8-amino nitrogen substitution on serotonin receptor binding and pharmacology. |
Upjohn Laboratories |
| 7783131 |
78 |
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. |
H. Lundbeck |
| 7799409 |
20 |
Derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl-p-iodobenzamido)ethyl]pipera zine (p-MPPI) as 5-HT1A ligands. |
University of Pennsylvania |
| 8064803 |
43 |
Structure-affinity relationship studies on 5-HT1A receptor ligands. 2. Heterobicyclic phenylpiperazines with N4-aralkyl substituents. |
Solvay Duphar Research Laboratories |
| 8064801 |
232 |
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
University of G£Teborg |
| 7912735 |
270 |
3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
Universit£ |
| 8182697 |
11 |
Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand. |
University of Pennsylvania |
| 8289183 |
24 |
Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes. |
Abbott Laboratories |
| 7902439 |
31 |
(R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment. |
Asahi Chemical Industry |
| 8230131 |
25 |
Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
Medicinaregatan |
| 8230102 |
21 |
Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. |
University of Pennsylvania |
| 1346653 |
168 |
Pyrrole mannich bases as potential antipsychotic agents. |
R. W. Johnson Pharmaceutical Research Institute |
| 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 |
| 1995871 |
25 |
A 3-D model for 5-HT1A-receptor agonists based on stereoselective methyl-substituted and conformationally restricted analogues of 8-hydroxy-2-(dipropylamino)tetralin. |
Uppsala University |
| 1833546 |
47 |
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands. |
Abbott Laboratories |
| 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 |
| 2569041 |
8 |
5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine. |
College of Pharmacy University of Iowa |
| 2542551 |
89 |
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
Bristol-Myers |
| 2565399 |
25 |
Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents. |
Wyeth-Ayerst Research |
| 2539480 |
50 |
Design and synthesis of propranolol analogues as serotonergic agents. |
Virginia Commonwealth University |
| 2571729 |
15 |
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties. |
University of G£Teborg |
| 2898533 |
50 |
Polycyclic aryl- and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies. |
Wyeth-Ayerst Research |
| 2967376 |
13 |
Central dopaminergic and 5-hydroxytryptaminergic effects of C3-methylated derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin. |
University of Uppsala |
| 3543362 |
184 |
Central serotonin receptors as targets for drug research. |
TBA |
| 11078200 |
61 |
N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists. |
Welfide |
| 9873481 |
80 |
SAR of novel biarylmethylamine dopamine D4 receptor ligands. |
Darmstadt |
| 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 |
| 21859099 |
57 |
Optimization of (arylpiperazinylbutyl)oxindoles exhibiting selective 5-HT7 receptor antagonist activity. |
Egis Pharmaceuticals |
| 21802308 |
29 |
Synthesis and molecular modeling of 1H-pyrrolopyrimidine-2,4-dione derivatives as ligands for thea1-adrenoceptors. |
Universit£ |
| 21601317 |
47 |
Synthesis and structural investigation of some pyrimido[5,4-c]quinolin-4(3H)-one derivatives with a long-chain arylpiperazine moiety as potent 5-HT(1A/2A) and 5-HT(7) receptor ligands. |
Medical University of Lodz |
| 21440338 |
36 |
Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents. |
Universit£ |
| 21093118 |
32 |
Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. part 3. |
Medical University of Warsaw |
| 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 |
| 20138771 |
34 |
SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. |
Universit£ |
| 19679379 |
33 |
Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
Jagiellonian University Medical College |
| 19665823 |
38 |
Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
Medical University of Warsaw |
| 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 |
| | 48 |
Novel pyridazino[4,5-b][1,5]oxazepines and -thiazepines as 5-HT1A receptor ligands |
TBA |
| | 53 |
5-HT1A and 5-HT2A ligands with anxiolytic and antipanic-like properties |
TBA |
| | 12 |
The synthesis and evaluation of the major metabolites of mazapertine |
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 |
| | 12 |
5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonist |
TBA |
| | 34 |
Bivalent indoles exhibiting serotonergic binding affinity |
TBA |
| | 68 |
N-(2-pyrrolidinylmethyl)benzoxazine-8-carboxamides exhibiting high affinities for All of D2, 5-HT1 A, and 5-HT2 receptors |
TBA |
| | 25 |
Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic properties |
TBA |
| | 50 |
Synthesis and evaluation of n-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives as potential anti-ischemic agents |
TBA |
| | 29 |
Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile |
TBA |
| | 17 |
C8-substituted derivatives of 2-(dipropylamino)tetralin: Palladium-catalyzed synthesis and interactions with 5-HT1A-receptors |
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) |
| 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 |
| 18995929 |
24 |
Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity, part 1. |
Medical University of Warsaw |
| 18835172 |
19 |
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities. |
Chinese Academy of Sciences |
| 18783955 |
35 |
N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands. |
Chinese Academy of Sciences |
| 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 |
| 18598015 |
53 |
Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands. |
Università |
| 18585036 |
18 |
Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines. |
Harvard Medical School |
| 18562201 |
13 |
Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines. |
Chinese Academy of Sciences |
| 18487050 |
36 |
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter. |
Hadassah Hebrew University Hospital |
| 18486277 |
58 |
Synthesis and serotonin receptor activity of the arylpiperazine alkyl/propoxy derivatives of new azatricycloundecanes. |
Institute of Pharmacology of The Polish Academy of Sciences |
| 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 |
| 17419056 |
16 |
Novel aminoethylbiphenyls as 5-HT7 receptor ligands. |
Université |
| 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 |
| 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 |
| 16545955 |
16 |
New 4-(4-methyl-phenyl)phthalazin-1(2H)-one derivatives and their effects on alpha1-receptors. |
Università |
| 16250661 |
13 |
11C-labeling of n-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors. |
University of Milano/Bicocca |
| 16219465 |
82 |
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs. |
Abbott |
| 16107148 |
44 |
New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation. |
Università |
| 16055331 |
45 |
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
Carlsson Research |
| 16002287 |
9 |
Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands. |
Université |
| 15801833 |
35 |
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands. |
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 |
| 15501057 |
20 |
The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands. |
Polish Academy of Sciences |
| 15341484 |
159 |
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors. |
Merck |
| 15341483 |
110 |
Indolebutylamines as selective 5-HT(1A) agonists. |
Merck |
| 15267230 |
50 |
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists. |
Uppsala University |
| 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 |
| 12951088 |
22 |
Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands. |
Universidad Complutense |
| 12877594 |
14 |
Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety. |
Università |
| 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 |
| 12482417 |
23 |
alpha1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus. |
Università |
| 12213056 |
42 |
Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
Universidad De Navarra |
| 12166933 |
24 |
Alpha(1)-adrenoceptor antagonists. 4. Pharmacophore-based design, synthesis, and biological evaluation of new imidazo-, benzimidazo-, and indoloarylpiperazine derivatives. |
Università |
| 11934576 |
85 |
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands. |
Université |
| 11741489 |
45 |
Dopamine D(3) receptor antagonists. 1. Synthesis and structure-activity relationships of 5,6-dimethoxy-N-alkyl- and N-alkylaryl-substituted 2-aminoindans. |
Pharmacia |
| 11728188 |
53 |
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
Università |
| 11689074 |
112 |
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands. |
Merck Sharp & Dohme Research Laboratories |
| 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 |
| 11229779 |
11 |
New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects. |
Suntory Biomedical Research |
| 11212112 |
24 |
Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives. |
Uppsala University |
| 11101361 |
37 |
Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
Purdue University |
| 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 |
| 10853650 |
36 |
Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. |
Yoshitomi Pharmaceutical Industries |
| 10843224 |
28 |
High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor. |
Università |
| 10753471 |
64 |
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors. |
Uppsala University |
| 10743959 |
48 |
N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. |
Yoshitomi Pharmaceutical Industries |
| 10737747 |
54 |
5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants. |
Merck |
| 10669578 |
44 |
New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides. |
University of Groningen |
| 10669570 |
8 |
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
University of Groningen |
| 10649982 |
54 |
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand. |
Universitá |
| 10636243 |
6 |
Synthesis and binding studies of some epibatidine analogues. |
Institute of Pharmacy and Biochemistry |
| 10585205 |
10 |
On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists. |
Polish Academy of Sciences |
| 10476865 |
2 |
Synthesis of new (benzimidazolyl)piperazines with affinity for the 5-HT1A receptor via Pd(0) amination of bromobenzimidazoles. |
Universidad Complutense |
| 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 |
| 10386940 |
31 |
Novel derivatives of 3-(dipropylamino)chroman. Interactions with 5-HT1A and D2A receptors. |
Uppsala University |
| 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 |
| 10354409 |
131 |
New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template. |
Wyeth-Ayerst Research Laboratories |
| 10090793 |
12 |
Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine. |
Purdue University |
| 9986719 |
39 |
1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5. |
Università |
| 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 |
| 9934472 |
12 |
Phenylpiperazine derivatives with strong affinity for 5HT1A, D2A and D3 receptors. |
University of Vigo |
| 9888842 |
21 |
Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton. |
Università |
| 9888831 |
83 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. 4. 1-[omega-(4-Arylpiperazin-1-yl)alkyl]-3-(diphenylmethylene) - 2, 5-pyrrolidinediones and -3-(9H-fluoren-9-ylidene)-2, 5-pyrrolidinediones: study of the steric requirements of the terminal amide fragment on 5-HT1A a |
Universidad Complutense |
| 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 |
| 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 |
| 9873563 |
67 |
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists. |
Merck |
| 9871719 |
144 |
Serotonergic ergoline derivatives. |
Pharmacia & Upjohn |
| 9871564 |
60 |
1-[omega-(4-arylpiperazin-1-yl)alkyl]-3-diphenylmethylene-2,5- pyrrolidinediones as 5-HT1A receptor ligands: study of the steric requirements of the terminal amide fragment on 5-HT1A affinity/selectivity. |
Universidad Complutense |
| 9836624 |
64 |
Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding. |
Virginia Commonwealth University |
| 9836617 |
30 |
Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives. |
Purdue University |
| 9822559 |
47 |
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand. |
Universitá |
| 9667967 |
65 |
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists. |
Yamanouchi Pharmaceutical |
| 9622555 |
25 |
Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity. |
Purdue University |
| 9513604 |
76 |
Aminopyrimidines with high affinity for both serotonin and dopamine receptors. |
Warner-Lambert |
| 9457239 |
18 |
Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands. |
University of Pennsylvania |
| 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 |
| 9258372 |
40 |
Synthesis and structure-activity relationships of a new model of arylpiperazines. 3.1 2-[omega-(4-arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: study of the influence of the terminal amide fragment on 5-HT1A affinity/selectivity. |
Universidad Complutense |
| 9046348 |
45 |
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands. |
Università |
| 9022796 |
57 |
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines. |
Solvay Pharma |
| 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 |
| 8893836 |
50 |
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists. |
Uppsala University |
| 8863806 |
68 |
3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans] |
Université |
| 8784448 |
63 |
11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions. |
Uppsala University |
| 8784447 |
63 |
10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions. |
Uppsala University |
| 31547945 |
88 |
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives. |
Cracow University of Technology |
| 8759640 |
61 |
Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships. |
Warner-Lambert |
| 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 |
| 8691438 |
48 |
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
Pharmacia & Upjohn |
| 8676348 |
10 |
8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as buspirone. |
Polish Academy of Sciences |
| 8667368 |
42 |
Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist. |
University of Camerino |
| 8568802 |
42 |
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. |
Glaxo Wellcome |
| 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) |
| 8410989 |
58 |
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents. |
Solvay Duphar Research Laboratories |
| 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 |
| 8340910 |
32 |
(S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
University of GöTeborg |
| 8289207 |
30 |
Mixed 5-HT1A/D-2 activity of a new model of arylpiperazines: 1-aryl-4-[3-(1,2-dihydronaphthalen-4-yl)-n-propyl]piperazines. 1. Synthesis and structure-activity relationships. |
Università |
| 24531229 |
62 |
New 1-arylindoles based serotonin 5-HT7 antagonists. Synthesis and binding evaluation studies. |
Universit£ |
| 8246239 |
84 |
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives. |
Solvay Duphar |
| 8064802 |
9 |
Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new putative 5-HT1A receptor antagonist, and its analogs. |
Polish Academy of Sciences |
| 8057297 |
24 |
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
Pfizer |
| 23902232 |
42 |
6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective ?1D-adrenoceptor antagonist. |
Universit£ |
| 7996545 |
3 |
1-(2,5-Dimethoxy-4-(trifluoromethyl)phenyl)-2-aminopropane: a potent serotonin 5-HT2A/2C agonist. |
Purdue University |
| 7990123 |
30 |
Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors. |
University of Pennsylvania |
| 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 |
| 7932553 |
42 |
6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
GöTeborg University |
| 7914539 |
36 |
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
Burroughs Wellcome |
| 7914536 |
96 |
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
Hoechst-Roussel Pharmaceuticals |
| 7909336 |
27 |
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
R. W. Johnson Pharmaceutical Research Institute |
| 7861420 |
62 |
C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
Upjohn Laboratories |
| 7861413 |
11 |
(R)-11-hydroxy- and (R)-11-hydroxy-10-methylaporphine: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions. |
Uppsala University |
| 7783152 |
170 |
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
GöTeborg University |
| 7783126 |
29 |
N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands. |
Solvay Duphar Research Laboratories |
| 7752194 |
5 |
Buspirone analogues as ligands of the 5-HT1A receptor. 1. The molecular structure of buspirone and its two analogues. |
Pharmaceutical Research Institute |
| 7731013 |
32 |
New (2-methoxyphenyl)piperazine derivatives as 5-HT1A receptor ligands with reduced alpha 1-adrenergic activity. Synthesis and structure-affinity relationships. |
Faes |
| 7699712 |
20 |
Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes. |
Purdue University |
| 7699710 |
84 |
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2. |
Università |
| 7530773 |
31 |
Derivatives of cis-2-amino-8-hydroxy-1-methyltetralin: mixed 5-HT1A-receptor agonists and dopamine D2-receptor antagonists. |
Uppsala University |
| 7506312 |
36 |
Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors. |
Uppsala University |
| 17129726 |
121 |
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
| 17870534 |
21 |
Two new phenylpiperazines with atypical antipsychotic potential. |
Institute For Biological Research |
| 17803293 |
44 |
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
Pierre Fabre Research Center |
| 17300168 |
81 |
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
Pierre Fabre Research Center |
| 10229633 |
130 |
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. |
Pierre Fabre Research Center |
| 10411472 |
6 |
Synthesis and serotonergic activity of substituted 2, N-benzylcarboxamido-5-(2-ethyl-1-dioxoimidazolidinyl)-N, N-dimethyltryptamine derivatives: novel antagonists for the vascular 5-HT(1B)-like receptor. |
Monash University (Parkville Campus) |
| 9836623 |
71 |
Design and synthesis of a series of 6-substituted-2-pyridinylmethylamine derivatives as novel, high-affinity, selective agonists at 5-HT1A receptors. |
Pierre Fabre Research Center |
| 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 |
| 8917649 |
60 |
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist. |
University of Camerino |
| 8568799 |
281 |
Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models. |
Universit£ |
| 7473558 |
12 |
A series of N4-imidoethyl derivatives of 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A receptor ligands: synthesis and structure-affinity relationships. |
Solvay Duphar Research Laboratories |
| 8057272 |
33 |
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists. |
Glaxo Research and Development |
| 30383372 |
190 |
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
Huazhong University of Science and Technology |
| 3172131 |
23 |
Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands. |
Virginia Commonwealth University |
| 29767995 |
34 |
Structure-Activity Relationships and Therapeutic Potentials of 5-HT |
Universit£ |
| 29730027 |
99 |
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system. |
Jagiellonian University Medical College |
| 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 |
| 29269256 |
38 |
5-HT |
Medical University of Warsaw |
| 2902227 |
10 |
Serotonergic properties of spiroxatrine enantiomers. |
University of Arizona |
| 29138029 |
21 |
Synthesis and antidepressant activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HT |
Shanghai Institute of Pharmaceutical Industry |
| 28943244 |
136 |
New 5-HT |
Dipartimento Di Farmacia Universit£ |
| 2795604 |
3 |
(R)- and (S)-5,6,7,8-tetrahydro-1-hydroxy-N,N-dipropyl-9H-benzocyclohepten- 8-ylamine. Stereoselective interactions with 5-HT1A receptors in the brain. |
University of Uppsala |
| 2754715 |
24 |
N-(phthalimidoalkyl) derivatives of serotonergic agents: a common interaction at 5-HT1A serotonin binding sites? |
Virginia Commonwealth University |
| 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 |
| 2522991 |
8 |
Resolved N,N-dialkylated 2-amino-8-hydroxytetralins: stereoselective interactions with 5-HT1A receptors in the brain. |
University of Uppsala |
| 2521252 |
15 |
2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. |
Virginia Commonwealth University |
| 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 |
| 28575721 |
48 |
Synthesis of a new series of aryl/heteroarylpiperazinyl derivatives of 8-acetyl-7-hydroxy-4-methylcoumarin with low nanomolar 5-HT |
Medical University of Warsaw |
| 2140413 |
6 |
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist. |
TBA |
| 2137880 |
7 |
Novel [(diazomethyl)carbonyl]-1,2,3,4-tetrahydronaphthalene derivatives as potential photoaffinity ligands for the 5-HT1A receptor. |
Mount Sinai School of Medicine |
| 1977911 |
1 |
Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines. |
Asahi Chemical Industry |
| 1732537 |
3 |
Stereoselective LSD-like activity in d-lysergic acid amides of (R)- and (S)-2-aminobutane. |
Purdue University |
| 1683407 |
32 |
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 1676427 |
21 |
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
Pfizer |
| 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 |
| 1648138 |
33 |
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands. |
Universitá |
| 1535661 |
24 |
Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site. |
Polish Academy of Sciences |
| 1534585 |
8 |
Benzofuran bioisosteres of hallucinogenic tryptamines. |
Purdue University |
| 1433207 |
22 |
6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. |
University of GöTeborg |
| 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 |
| 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 |
| 9089668 |
95 |
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. |
Northwestern University |
| 9067310 |
20 |
Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats. |
Institut De Recherches Servier |
| 12857114 |
102 |
High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II. |
Uppsala University |
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