139 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
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
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
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
(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
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
Institut De Pharmacologie (Ua 589 Cnrs)
Alkylating prazosin analogue: irreversible label for alpha 1-adrenoceptors.
National Institute On Aging/Grc
Indoline analogues of idazoxan: potent alpha 2-antagonists and alpha 1-agonists.
Reckitt and Colman
1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential alpha 1-adrenoceptor antagonists.
Pfizer
2,4-Diamino-6,7-dimethoxyquinoline derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Pfizer
2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-[4-(substituted oxyethoxy) piperidino] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Pfizer
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
TBA
Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives.
TBA
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
TBA
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
2,4-Diamino-6,7-dimethoxyquinazolines. 3. 2-(4-Heterocyclylpiperazin-1-yl) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Pfizer
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
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
TBA
Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at alpha 1 and alpha 2 adrenergic receptors.
TBA
Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
TBA
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
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
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
TBA
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
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
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.
TBA
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.
TBA
(alpha S)-erythro-alpha-methylepinephrine: preparation and stereoselective binding to adrenergic receptors in rat forebrain.
TBA
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.
TBA
Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists.
Pfizer
alpha(1)-Adrenoceptor antagonists. Rational design, synthesis and biological evaluation of new trazodone-like compounds.
University of Pisa
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
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.
Glaxosmithkline
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
Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives.
University of Pisa
Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans.
H. Lundbeck
Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.
University of Pisa
Pyrrole mannich bases as potential antipsychotic agents.
R. W. Johnson Pharmaceutical Research Institute
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
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.
Centre De Recherches De Vitry Alfortville Rh£Ne-Poulenc Rorer
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
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.
Warner-Lambert
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity.
Bristol-Myers
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.
H. Lundbeck
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
TBA
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
Duphar Research Laboratories
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
TBA
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
TBA
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Eli Lilly
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
University of Siena
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
1-(2-METHOXYPHENYL)-4-ALKYLPIPERAZINES: EFFECT OF THE N-4 SUBSTITUENT ON THE AFFINITY AND SELECTIVITY FOR DOPAMINE D4 RECEPTOR
TBA
2-[4-(o-methoxyphenyl)piperazin-1-ylmethyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine as a new selective 5-HT1A receptor ligand
TBA
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
Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton.
Northwest University
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
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
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
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
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
Development of a presynaptic 5-HT1A antagonist.
Bristol-Myers Squibb Pharmaceutical Research Institute
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
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
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
Novel Aryloxyethyl Derivatives of 1-(1-Benzoylpiperidin-4-yl)methanamine as the Extracellular Regulated Kinases 1/2 (ERK1/2) Phosphorylation-Preferring Serotonin 5-HT
Jagiellonian University Medical College
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
Synthesis and biological evaluation of novel antipsychotic trans-4-(2-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)ethyl)cyclohexan-1-amine derivatives targeting dopamine/serotonin receptor subtypes.
Shanghai Institute of Pharmaceutical Industry
Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HT
Janssen Research & Development
Discovery of Novel pERK1/2- or ?-Arrestin-Preferring 5-HT
Jagiellonian University Medical College
Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors.
Wyeth-Ayerst Research Laboratories
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.
University of Crete
Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity.
Yoshitomi Pharmaceutical Industries
High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor.
Università
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
Università
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
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
Merck
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
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
R. W. Johnson Pharmaceutical Research Institute
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
(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)
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
Eli Lilly
Fluorinated analogues of marsanidine, a highly ?2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities.
Medical University of Gdansk
Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT? receptor.
University of Bari Aldo Moro
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
Jagiellonian University Medical College
Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone.
Jagiellonian University Medical College
Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with ??-adrenoceptor antagonistic properties.
Jagiellonian University Medical College
Antiarrhythmic properties of phenylpiperazine derivatives of phenytoin with ??-adrenoceptor affinities.
Jagiellonian University Medical College
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
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
Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action.
Universidad De Chile
Comparative study of the vasodilatory effects of three quinazoline alkaloids isolated from Evodia rutaecarpa.
National Research Instituter of Chinese Medicine
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
Solvay Pharma
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.
Merck Sharp and Dohme Research Laboratories
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Merck Research Laboratories
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
Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties.
Institut De Recherches Servier
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.
University of Perugia
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.
Combichem
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
Pierre Fabre Research Center
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
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.
Monash University
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
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ohio State University
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses.
Pfizer
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Huazhong University of Science and Technology
Troponoids. 7. Chemistry and dopamine agonist activity of ciladopa and related aralkyltroponylpiperazines.
TBA
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.
TBA
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
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
Duphar Research Laboratories
Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives.
Bristol-Myers
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
Warner-Lambert
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
TBA
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
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT
Jagiellonian University Medical College
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
Jagiellonian University Medical College
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
Bristol-Myers Squibb Pharmaceutical Research Institute
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.
Pfizer
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
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
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
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
H. Lundbeck
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.
Upjohn