The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 8101878 |
61 |
Studies on quinazolines. 5. 2,3-dihydroimidazo[1,2-c]quinazoline derivatives: a novel class of potent and selective alpha 1-adrenoceptor antagonists and antihypertensive agents. |
National Defense Medical Center |
| 1347319 |
15 |
Synthesis and alpha-adrenergic activities of 2- and 4-substituted imidazoline and imidazole analogues. |
Ohio State University |
| 1671705 |
126 |
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors. |
Syntex Research |
| 2153820 |
86 |
Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha 2-adrenoceptor vs the [3H]yohimbine-labeled site. |
Syntex Research |
| 2570150 |
10 |
(8a alpha,12a alpha,13a alpha)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridi ne, a potent and highly selective alpha 2-adrenoceptor antagonist. |
Syntex Research |
| 2542561 |
48 |
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties. |
Institut De Pharmacologie (Ua 589 Cnrs) |
| 2535878 |
32 |
Alkylating prazosin analogue: irreversible label for alpha 1-adrenoceptors. |
National Institute On Aging/Grc |
| 2896247 |
14 |
Indoline analogues of idazoxan: potent alpha 2-antagonists and alpha 1-agonists. |
Reckitt and Colman |
| 2896246 |
5 |
1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential alpha 1-adrenoceptor antagonists. |
Pfizer |
| 2896245 |
19 |
2,4-Diamino-6,7-dimethoxyquinoline derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
Pfizer |
| 2894465 |
18 |
2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-[4-(substituted oxyethoxy) piperidino] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
Pfizer |
| 2887657 |
52 |
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines. |
TBA |
| 3039138 |
23 |
Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives. |
TBA |
| 2884316 |
34 |
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
TBA |
| 2884313 |
10 |
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors. |
TBA |
| 2888896 |
20 |
2,4-Diamino-6,7-dimethoxyquinazolines. 3. 2-(4-Heterocyclylpiperazin-1-yl) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
Pfizer |
| 2879919 |
21 |
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
TBA |
| 3016265 |
94 |
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors. |
TBA |
| 2870187 |
20 |
Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at alpha 1 and alpha 2 adrenergic receptors. |
TBA |
| 2876101 |
18 |
Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists. |
TBA |
| 2863377 |
10 |
6,7-Dihydro-5-[[(cis-2-hydroxy-trans-3-phenoxycyclopentyl)amino] methyl]-2-methylbenzo[b]thiophen-4(5H)-one: a novel alpha 1-adrenergic receptor antagonist and renal vasodilator. |
TBA |
| 2989524 |
51 |
Synthesis, in vitro [3H]prazosin displacement, and in vivo activity of 3-aryl-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridines, a new class of antihypertensive agents. |
TBA |
| 3973904 |
30 |
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
TBA |
| 2866248 |
8 |
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
TBA |
| 2999398 |
2 |
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral alpha-adrenoreceptors. |
TBA |
| 4045929 |
30 |
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
TBA |
| 2864446 |
66 |
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes. |
TBA |
| 6133954 |
6 |
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones. |
TBA |
| 6131130 |
58 |
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives. |
TBA |
| 6124637 |
18 |
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols. |
TBA |
| 6123600 |
10 |
1-(alkylamino)isochromans: hypotensives with peripheral and central activities. |
TBA |
| 7328589 |
8 |
(alpha S)-erythro-alpha-methylepinephrine: preparation and stereoselective binding to adrenergic receptors in rat forebrain. |
TBA |
| 7328588 |
9 |
Synthesis and adrenoceptor affinity of some highly polar beta-substituted catecholamines. |
TBA |
| 6249933 |
12 |
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues. |
TBA |
| 6248642 |
38 |
Mammalian alkaloids. 8. Synthesis and biological effects of tetrahydropapaveroline related 1-benzyltetrahydroisoquinolines. |
TBA |
| 12482437 |
42 |
Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists. |
Pfizer |
| 11814815 |
13 |
alpha(1)-Adrenoceptor antagonists. Rational design, synthesis and biological evaluation of new trazodone-like compounds. |
Universit£ |
| 27709945 |
62 |
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea |
Chinese Academy of Sciences |
| 26238322 |
26 |
Indolylpiperidine derivatives as potent and selectivea1B adrenoceptor antagonists. |
Toray Industries |
| 11462977 |
21 |
Analogues of prazosin that bear a benextramine-related polyamine backbone exhibit different antagonism toward alpha1-adrenoreceptor subtypes. |
University of Bologna |
| 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 |
| 12419381 |
95 |
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
Glaxosmithkline |
| 20934789 |
27 |
Synthesis anda1-adrenoceptor antagonist activity of tamsulosin analogues. |
Universit£ |
| 20813529 |
48 |
Search for influence of spatial properties on affinity ata1-adrenoceptor subtypes for phenylpiperazine derivatives of phenytoin. |
Jagiellonian University Medical College |
| 19719240 |
25 |
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity. |
University of Camerino |
| 9548813 |
53 |
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. |
Smithkline Beecham Pharmaceuticals |
| 21486038 |
177 |
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. |
H. Lundbeck |
| 21549456 |
10 |
Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-adrenergic receptor blocking properties. |
Universidade Federal Do Rio De Janeiro |
| 23124215 |
72 |
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selectivea1B-adrenoceptor antagonist. |
Universit£ |
| 16723224 |
26 |
Design and synthesis of selective alpha1B adrenoceptor antagonists. |
Toray Industries |
| 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£ |
| 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 |
| 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£ |
| 10602703 |
73 |
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent. |
Warner-Lambert |
| 10579843 |
81 |
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series. |
Synaptic Pharmaceutical |
| 10579840 |
88 |
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones. |
Synaptic Pharmaceutical |
| 10447960 |
20 |
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography. |
Universidad De Valencia |
| 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 |
| 9135028 |
114 |
Pharmacological options in the treatment of benign prostatic hyperplasia. |
Pfizer |
| 8254623 |
54 |
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 8230093 |
34 |
Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives. |
Universit£ |
| 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 |
| 1313109 |
40 |
Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors. |
Universit£ |
| 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 |
| 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 |
| 1671416 |
15 |
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones. |
Warner-Lambert |
| 1976813 |
83 |
2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: synthesis and antidepressant activity. |
Wyeth-Ayerst Research |
| 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 |
| 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 |
| 6142954 |
70 |
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
TBA |
| 6139481 |
32 |
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines. |
TBA |
| 15109634 |
129 |
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis. |
Eli Lilly |
| 11354357 |
61 |
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien. |
Abbott Laboratories |
| 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£ |
| 19762239 |
18 |
Structure-activity relationship study on alpha1 adrenergic receptor antagonists from beer. |
University of Shizuoka and Global Coe Program |
| 19788200 |
7 |
Further studies on arylpiperazinyl alkyl pyridazinones: discovery of an exceptionally potent, orally active, antinociceptive agent in thermally induced pain. |
Dipartimento Di Scienze Farmaceutiche |
| 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 |
| | 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 |
| | 33 |
1-(2-METHOXYPHENYL)-4-ALKYLPIPERAZINES: EFFECT OF THE N-4 SUBSTITUENT ON THE AFFINITY AND SELECTIVITY FOR DOPAMINE D4 RECEPTOR |
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 |
| | 14 |
Marine sponge bis(indole) alkaloids that displace ligand binding to α1 adrenergic receptors |
TBA |
| | 14 |
Oxindole N-Methyl-D-Aspartate (NMDA) antagonists |
TBA |
| 18160289 |
119 |
1-Aminoindanes as novel motif with potential atypical antipsychotic properties. |
Pfizer |
| 17976986 |
80 |
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
Pfizer |
| 16722631 |
87 |
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
Predix Pharmaceuticals |
| 16513345 |
45 |
Vasorelaxant activity of phthalazinones and related compounds. |
Universidad De Salamanca |
| 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 |
| 15055991 |
265 |
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor. |
Recordati |
| 14698193 |
43 |
Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane. |
Wyeth Research |
| 12951084 |
8 |
1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists. |
F. Hoffmann-La Roche |
| 12729659 |
29 |
4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists. |
F. Hoffmann-La Roche |
| 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 |
| 12639562 |
41 |
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist. |
Neurogen |
| 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 |
| 12372513 |
102 |
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation. |
Neurogen |
| 12372512 |
239 |
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships. |
Neurogen |
| 12361399 |
17 |
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding. |
Universita Di Camerino |
| 12238918 |
22 |
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine. |
Abbott Laboratories |
| 11814784 |
53 |
Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors. |
Wyeth-Ayerst Research Laboratories |
| 11459653 |
31 |
Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors. |
Wyeth-Ayerst Research Laboratories |
| 11384242 |
126 |
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia. |
Abbott Laboratories |
| 11294383 |
16 |
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies. |
University of Crete |
| 10956183 |
19 |
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability. |
Synaptic Pharmaceutical |
| 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 |
| 10780916 |
134 |
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH). |
Abbott Laboratories |
| 10743949 |
76 |
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents. |
Università |
| 10715142 |
35 |
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor. |
The R. W. Johnson Pharmaceutical Research Institute |
| 10021947 |
44 |
4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists. |
Merck |
| 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 |
| 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 |
| 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 |
| 9871525 |
56 |
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors. |
R. W. Johnson Pharmaceutical Research Institute |
| 9572880 |
44 |
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand. |
University of Camerino |
| 9548811 |
55 |
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist. |
Merck |
| 9379432 |
36 |
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign pr |
Abbott Laboratories |
| 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 |
| 8809161 |
90 |
Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole. |
H. Lundbeck |
| 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 |
| 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) |
| 8411007 |
392 |
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
Mayo Foundation |
| 8410999 |
81 |
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
Eli Lilly |
| 25282262 |
39 |
Fluorinated analogues of marsanidine, a highly ?2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities. |
Medical University of Gdansk |
| 42798 |
4 |
Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some alpha-adrenergic benzylimidazolines. |
TBA |
| 231654 |
16 |
Synthesis and biological properties of 2-, 5-, and 6-fluoronorepinephrines. |
TBA |
| 17749 |
5 |
Absolute configuration of glycerol derivatives. 4. Synthesis and pharmacological activity of chiral 2-alkylaminomethylbenzodioxans, competitive alpha-adrenergic antagonists. |
TBA |
| 24508140 |
59 |
Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT? receptor. |
Universit£ |
| 23787101 |
33 |
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety. |
Jagiellonian University Medical College |
| 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 |
| 23245804 |
17 |
Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone. |
Jagiellonian University Medical College |
| 7658428 |
94 |
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. |
Smithkline Beecham Pharmaceuticals |
| 22739084 |
15 |
Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with ??-adrenoceptor antagonistic properties. |
Jagiellonian University Medical College |
| 22381672 |
20 |
Antiarrhythmic properties of phenylpiperazine derivatives of phenytoin with ??-adrenoceptor affinities. |
Jagiellonian University Medical College |
| 21232965 |
5 |
Pharmacophore models based studies on the affinity and selectivity toward 5-HT1A with reference to ?1-adrenergic receptors among arylpiperazine derivatives of phenytoin. |
Jagiellonian University Medical College |
| 19647907 |
16 |
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2. |
Rzesz£W University of Technology |
| 12880313 |
33 |
Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action. |
Universidad De Chile |
| 8699182 |
1 |
Comparative study of the vasodilatory effects of three quinazoline alkaloids isolated from Evodia rutaecarpa. |
National Research Instituter of Chinese Medicine |
| 17880057 |
131 |
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
Solvay Pharma |
| 16337790 |
53 |
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands. |
Merck Sharp and Dohme Research Laboratories |
| 15056006 |
69 |
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. |
Merck Research Laboratories |
| 15163201 |
189 |
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist. |
Abbott Laboratories |
| 11754589 |
68 |
Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. |
Institut De Recherches Servier |
| 11262089 |
213 |
Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties. |
Institut De Recherches Servier |
| 6192241 |
15 |
Synthesis and biological properties of thiophene ring analogues of mianserin. |
TBA |
| 11405649 |
118 |
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors. |
Universit£ |
| 10893315 |
7 |
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists. |
Combichem |
| 10229633 |
130 |
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. |
Pierre Fabre Research Center |
| 9301663 |
28 |
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket". |
University of Tennessee |
| 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 |
| 8831777 |
48 |
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist. |
Abbott Laboratories |
| 8709134 |
26 |
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine. |
Ohio State University |
| 7636876 |
20 |
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses. |
Pfizer |
| 30383372 |
190 |
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
Huazhong University of Science and Technology |
| 3950903 |
12 |
Troponoids. 7. Chemistry and dopamine agonist activity of ciladopa and related aralkyltroponylpiperazines. |
TBA |
| 3746815 |
15 |
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin. |
TBA |
| 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 |
| 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 |
| 2894466 |
39 |
Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives. |
Bristol-Myers |
| 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 |
| 29425815 |
76 |
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT |
Jagiellonian University Medical College |
| 29128116 |
3 |
Design and synthesis of small molecule agonists of EphA2 receptor. |
Case Western Reserve University School of Medicine |
| 29706529 |
22 |
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone. |
Jagiellonian University Medical College |
| 29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 28958623 |
35 |
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H |
Glaxosmithkline |
| 1683407 |
32 |
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 1681106 |
27 |
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds. |
Pfizer |
| 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 |
| 1648138 |
33 |
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands. |
Universitá |
| 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 |
| 1323682 |
61 |
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor. |
Upjohn |
| 26943478 |
16 |
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives. |
Chulabhorn Research Institute |
| 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 |
| 26364932 |
22 |
Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity. |
University of North Carolina At Chapel Hill |
| 25590533 |
245 |
Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1. |
University of North Carolina At Chapel Hill |
| 10747922 |
12 |
Compulsory order of substrate binding to herpes simplex virus type 1 thymidine kinase. A calorimetric study. |
Swiss Federal Institute of Technology |
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