407 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Synthesis and alpha-adrenergic activities of 2- and 4-substituted imidazoline and imidazole analogues.
Ohio State University
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
Conformationally defined adrenergic agents. 4. 1-(aminomethyl)phthalans: synthesis and pharmacological consequences of the phthalan ring oxygen atom.
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
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral alpha-adrenoreceptors.
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
Synthesis and adrenoceptor affinity of some highly polar beta-substituted catecholamines.
TBA
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.
TBA
Mammalian alkaloids. 8. Synthesis and biological effects of tetrahydropapaveroline related 1-benzyltetrahydroisoquinolines.
TBA
Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists.
Pfizer
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
Roche Bioscience
alpha(1)-Adrenoceptor antagonists. Rational design, synthesis and biological evaluation of new trazodone-like compounds.
Universit£
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Glaxosmithkline
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Glaxosmithkline
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT
Universit£
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Synthesis and structure-activity relationships of novel arylpiperazines as potent antagonists ofa1-adrenoceptor.
University of Bras£Lia
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines asa
Jagiellonian University Medical College
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea
Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selectivea1A-Adrenoceptor Antagonists.
Chengdu University
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Activea1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.
Takeda Pharmaceutical
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Indolylpiperidine derivatives as potent and selectivea1B adrenoceptor antagonists.
Toray Industries
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Humanß3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.
Asahi Kasei Pharma
Human alpha1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines.
Unsw Australia
Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands ata<alpha>1 and 5-HT1A receptors.
Universit£
Discovery of Quinazoline-Based Fluorescent Probes toa1-Adrenergic Receptors.
Shandong University
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.
City University of New York
a-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
Jagiellonian University Medical College
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
High affinity ligands and potent antagonists for thea1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives.
Universit£
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Intra-Cellular Therapies
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives ina1-adrenergic and 5-HT1A receptor binding sites recognition.
University of Camerino
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
Universidade Federal De Goi£S
Discovery of novela1-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
H. Lundbeck
Analogues of prazosin that bear a benextramine-related polyamine backbone exhibit different antagonism toward alpha1-adrenoreceptor subtypes.
University of Bologna
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
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.
Glaxosmithkline
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
Glaxosmithkline
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
Glaxosmithkline
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
Glaxosmithkline
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergica1- and serotonine 5-HT1A receptors.
Universit£
Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands fora1-adrenoceptor subtypes.
Universit£
Rigid analogues of thea2-adrenergic blocker atipamezole: small changes, big consequences.
Pierre Fabre Research Center
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study.
Universit£
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
Universit£
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.
Glaxosmithkline
Design, synthesis and pharmacological evaluation of new 1-[3-(4-arylpiperazin-1-yl)-2-hydroxy-propyl]-3,3-diphenylpyrrolidin-2-one derivatives with antiarrhythmic, antihypertensive, and alpha-adrenolytic activity.
Jagiellonian University Medical College
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
University of Camerino
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
Glaxosmithkline
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.
Universit£
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Glaxosmithkline
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).
Universit£
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
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Organon Research and Development Group
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Smithkline Beecham Pharmaceuticals
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
The University of Sydney
Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists.
Suven Life Sciences
Rediocide A, an Insecticide, induces G-protein-coupled receptor desensitization via activation of conventional protein kinase C.
Chinese Academy of Sciences
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors.
University of Li£Ge
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
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selectivea1B-adrenoceptor antagonist.
Universit£
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
Glaxosmithkline
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.
The University of Sydney
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute of Mental Health
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
University of Sydney
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Pfizer
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Selective optimization of side activities: another way for drug discovery.
Prestwick Chemical
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
H. Lundbeck
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
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
Warner-Lambert
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
Synaptic Pharmaceutical
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
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Smithkline Beecham Pharmaceuticals
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
Synaptic Pharmaceutical
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.
Universit£
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.
Universit£
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
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.
Abbott Laboratories
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
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Eli Lilly
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Abbott Laboratories
N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists.
Welfide
Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.
Merck Research Laboratories
Design and synthesis of novel dihydropyridine alpha-1a antagonists.
Synaptic Pharmaceutical
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Merck
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£
Design, synthesis and in vitro evaluation of bridgehead fluoromethyl analogs of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) for the 5-HT(1A) receptor.
Vu University Medical Center
Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile.
Soochow University College of Pharmaceutical Sciences
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor.
Vu University Medical Center
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors.
University of Copenhagen
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute of Mental Health
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.
Hokkaido University
Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines.
National Institute of Diabetes and Digestive and Kidney Diseases
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
Further studies on arylpiperazinyl alkyl pyridazinones: discovery of an exceptionally potent, orally active, antinociceptive agent in thermally induced pain.
Dipartimento Di Scienze Farmaceutiche
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
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)
TBA
2-[4-(o-methoxyphenyl)piperazin-1-ylmethyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine as a new selective 5-HT1A receptor ligand
TBA
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists
TBA
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.
TBA
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Pfizer
Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.
Pfizer
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents.
Sinhgad College of Pharmacy
Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Johnson & Johnson Pharmaceutical Research and Development
(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).
Johnson & Johnson Pharmaceutical Research and Development
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
Johnson & Johnson Pharmaceutical Research and Development
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
Panjab University
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
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.
Florida A&M University
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Alcon Research
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.
Jagiellonian University Medical College
Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton.
Northwest University
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
Chungbuk National University
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
Lundbeck Research Usa
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
H. Lundbeck
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Janssen-Cilag
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Merck
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.
Recordati
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
Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Virginia Commonwealth University
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.
Cracow University of Technology
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.
Neurogen
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
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.
Southern Medical University
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
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
F. Hoffmann-La Roche
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
Jiangsu Ocean University
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
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.
Universita Di Camerino
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
Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.
Johnson & Johnson Pharmaceutical Research and Development
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
Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.
Johnson & Johnson Pharmaceutical Research and Development
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
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
Discovery of Novel pERK1/2- or ?-Arrestin-Preferring 5-HT
Jagiellonian University Medical College
Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist.
F. Hoffmann-La Roche
Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma.
Celgene
Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors.
Wyeth-Ayerst Research Laboratories
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.
Istituto Chimico Farmaceutico E Tossicologico
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
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.
University of Crete
The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology.
University of Perugia
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
Determination of the relative and absolute stereochemistry of a potent and alpha1A-selective adrenoceptor antagonist.
Synaptic Pharmaceutical
Novel heterocycles as selective alpha1-adrenergic receptor antagonists.
The R. W. Johnson Pharmaceutical Research Institute
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
Synaptic Pharmaceutical
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.
Merck
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.
Merck Research Laboratories
Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity.
Yoshitomi Pharmaceutical Industries
Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
The R. W. Johnson Pharmaceutical Research Institute
High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor.
Università
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.
The R. W. Johnson Pharmaceutical Research Institute
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
(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
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.
Synaptic Pharmaceutical
An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.
Marquette University
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Synaptic Pharmaceutical
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D
University of Pennsylvania
Design and synthesis of 2-[4-[4-(m-(ethylsulfonamido)-phenyl) piperazin-1-yl]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazole (EF-7412) using neural networks. A selective derivative with mixed 5-HT1A/D2 antagonist properties.
Universidad Complutense
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina At Chapel Hill
4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists.
Merck
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
University of Florida
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
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
Merck
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.
Wyeth-Ayerst Research Laboratories
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
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.
Synaptic Pharmaceutical
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
University of Camerino
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
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
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
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
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as ?1A/1D-AR subselective antagonists for BPH.
Jinan University
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)
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Mayo Foundation
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
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.
Astellas Pharma
Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some alpha-adrenergic benzylimidazolines.
TBA
Absolute configuration of glycerol derivatives. 4. Synthesis and pharmacological activity of chiral 2-alkylaminomethylbenzodioxans, competitive alpha-adrenergic antagonists.
TBA
Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT? receptor.
Universit£
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£
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
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
Jagiellonian University Medical College
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
Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone.
Jagiellonian University Medical College
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Smithkline Beecham Pharmaceuticals
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 pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
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
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
Universit£
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.
Merck Sharp and Dohme Research Laboratories
Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the involvement of alpha1D- and alpha1B-adrenoreceptor subtypes in the regulation of human PC-3 prostate
Universit£
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Glaxosmithkline
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
Glaxosmithkline
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Merck Research Laboratories
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
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.
University of Bologna
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Glaxosmithkline 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.
Universit£
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
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.
University of Bologna
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.
University of Camerino
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
New York University Medical 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
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
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
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.
Glaxo Research and Development
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, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives.
Luoyang Normal University
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
Identification of 3,4-dihydro-2H-thiochromene 1,1-dioxide derivatives with a phenoxyethylamine group as highly potent and selective ?
Takeda Pharmaceutical
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Novel naftopidil derivatives containing methyl phenylacetate and their blocking effects on ?
Guangzhou Medical University
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
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
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
Evaluation of the antidepressant therapeutic potential of isocyanine and pseudoisocyanine analogues of the organic cation decynium-22.
The Australian Nuclear Science and Technology Organisation
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
Universit£
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT
Universit£
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
Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent.
American Cyanamid
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
Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives.
Birla Institute of Technology
New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.
Universidade De Evora
Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1.
Max Planck Institute of Molecular Physiology
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.
Tehran University of Medical Sciences