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169 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Conformationally defined adrenergic agents. 4. 1-(aminomethyl)phthalans: synthesis and pharmacological consequences of the phthalan ring oxygen atom.EBI
TBA
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.EBI
Roche Bioscience
Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HTEBI
University of Modena and Reggio Emilia
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI
University of Kansas
Synthesis and structure-activity relationships of novel arylpiperazines as potent antagonists ofa1-adrenoceptor.EBI
University of Bras£Lia
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as SelectiveaEBI
Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selectivea1A-Adrenoceptor Antagonists.EBI
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.EBI
Takeda Pharmaceutical
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI
The Alexander Shulgin Research Institute
Indolylpiperidine derivatives as potent and selectivea1B adrenoceptor antagonists.EBI
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.EBI
Asahi Kasei Pharma
Human alpha1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines.EBI
Unsw Australia
Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands ata<alpha>1 and 5-HT1A receptors.EBI
University of Modena and Reggio Emilia
Discovery of Quinazoline-Based Fluorescent Probes toa1-Adrenergic Receptors.EBI
Shandong University
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.EBI
University of Missouri
High affinity ligands and potent antagonists for thea1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives.EBI
University of Catania
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.EBI
University of Camerino
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.EBI
Glaxosmithkline
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.EBI
Glaxosmithkline
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.EBI
Glaxosmithkline
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.EBI
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.EBI
Glaxosmithkline
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergica1- and serotonine 5-HT1A receptors.EBI
University of Modena and Reggio Emilia
From libraries to candidate: the discovery of new ultra long-acting dibasicß2-adrenoceptor agonists.EBI
Astrazeneca
Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands fora1-adrenoceptor subtypes.EBI
University of Catania
Synthesis anda1-adrenoceptor antagonist activity of tamsulosin analogues.EBI
University of Camerino
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study.EBI
University of Bari Aldo Moro
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.EBI
University of Modena and Reggio Emilia
Discovery of a new series of 5-HT1A receptor agonists.EBI
University of Modena and Reggio Emilia
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.EBI
University of Camerino
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.EBI
University of Camerino
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).EBI
University of Milan
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.EBI
Sanford-Burnham Medical Research Institute
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selectivea1B-adrenoceptor antagonist.EBI
University of Milan
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.EBI
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.EBI
National Institute of Mental Health
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.EBI
H. Lundbeck
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI
Hunter College and The Graduate Center of The City University of New York
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.EBI
Pfizer
Design and synthesis of selective alpha1B adrenoceptor antagonists.EBI
Toray Industries
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.EBI
Pfizer
Designed multiple ligands. An emerging drug discovery paradigm.EBI
Organon Laboratories
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.EBI
Pfizer
Selective optimization of side activities: another way for drug discovery.EBI
Prestwick Chemical
New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes.EBI
University of Catania
Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes.EBI
The R. W. Johnson Pharmaceutical Research Institute
From hit to lead. Analyzing structure-profile relationships.EBI
Universities of Lille
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.EBI
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.EBI
Synaptic Pharmaceutical
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.EBI
Smithkline Beecham Pharmaceuticals
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.EBI
Synaptic Pharmaceutical
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.EBI
Abbott Laboratories
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI
Virginia Commonwealth University
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.EBI
Abbott Laboratories
N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists.EBI
Welfide
Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.EBI
Merck Research Laboratories
Design and synthesis of novel dihydropyridine alpha-1a antagonists.EBI
Synaptic Pharmaceutical
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.EBI
Merck
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.EBI
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.EBI
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.EBI
Vu University Medical Center
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI
National Institute of Mental Health
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.EBI
Hokkaido University
 
Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptorEBI
TBA
 
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)EBI
TBA
 
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonistsEBI
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.EBI
TBA
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists.EBI
Pfizer
Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.EBI
Pfizer
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.EBI
Vanderbilt University
Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.EBI
Pharmaceutical Research Institute
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).EBI
Johnson & Johnson Pharmaceutical Research and Development
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
Glaxosmithkline
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).EBI
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).EBI
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.EBI
Johnson & Johnson Pharmaceutical Research and Development
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.EBI
Panjab University
Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis.EBI
University of Kansas
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.EBI
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.EBI
Jagiellonian University Medical College
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.EBI
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.EBI
Lundbeck Research Usa
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.EBI
H. Lundbeck
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.EBI
Janssen-Cilag
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.EBI
Merck
Indolebutylamines as selective 5-HT(1A) agonists.EBI
Merck
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.EBI
Pfizer
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.EBI
Cracow University of Technology
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.EBI
Neurogen
New potential uroselective NO-donor alpha1-antagonists.EBI
Università
The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.EBI
Southern Medical University
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.EBI
F. Hoffmann-La Roche
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.EBI
Jiangsu Ocean University
Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.EBI
Johnson & Johnson Pharmaceutical Research and Development
Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.EBI
Johnson & Johnson Pharmaceutical Research and Development
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.EBI
Shanghai Institute of Pharmaceutical Industry
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.EBI
Università
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.EBI
F. Hoffmann-La Roche
Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma.EBI
Celgene
Cyclic imides as potent and selective alpha-1A adrenergic receptor antagonists.EBI
Merck
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.EBI
Istituto Chimico Farmaceutico E Tossicologico
Determination of the relative and absolute stereochemistry of a potent and alpha1A-selective adrenoceptor antagonist.EBI
Synaptic Pharmaceutical
Novel heterocycles as selective alpha1-adrenergic receptor antagonists.EBI
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.EBI
Synaptic Pharmaceutical
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.EBI
Merck
Phenylacetamides as selective alpha-1A adrenergic receptor antagonists.EBI
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.EBI
Merck Research Laboratories
Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.EBI
The R. W. Johnson Pharmaceutical Research Institute
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.EBI
The R. W. Johnson Pharmaceutical Research Institute
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.EBI
Synaptic Pharmaceutical
An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.EBI
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.EBI
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.EBI
Synaptic Pharmaceutical
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DEBI
National Institute of Neurological Disorders and Stroke
Chemical manipulations on the 1,4-dioxane ring of 5-HTEBI
University of Camerino
4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists.EBI
Merck
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.EBI
University of Florida
Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.EBI
Università
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.EBI
Merck
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.EBI
Wyeth-Ayerst Research Laboratories
1,3-Dioxane as a scaffold for potent and selective 5-HTEBI
University of Modena and Reggio Emilia
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.EBI
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 prEBI
Abbott Laboratories
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI
University of Minnesota Twin Cities
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as ?1A/1D-AR subselective antagonists for BPH.EBI
Jinan University
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.EBI
Astellas Pharma
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.EBI
University of Milan
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.EBI
Smithkline Beecham Pharmaceuticals
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI
Drug Discovery Laboratory
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.EBI
University of Catania
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 prostateEBI
University of Camerino
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.EBI
University of Bologna
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.EBI
Glaxosmithkline Research Laboratories
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.EBI
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.EBI
University of Camerino
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.EBI
New York University Medical Center
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.EBI
University of Camerino
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.EBI
Glaxo Research and Development
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.EBI
Texas Tech University Health Sciences Center
Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives.EBI
Luoyang Normal University
Identification of 3,4-dihydro-2H-thiochromene 1,1-dioxide derivatives with a phenoxyethylamine group as highly potent and selective ?EBI
Takeda Pharmaceutical
Structure-Guided Modification of Heterocyclic Antagonists of the P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Novel naftopidil derivatives containing methyl phenylacetate and their blocking effects on ?EBI
Guangzhou Medical University
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI
University of Texas At Austin
Quinazoline based ?EBI
Alma Mater Studiorum-University of Bologna
Chiral analogues of (+)-cyclazosin as potent?EBI
University of Camerino
Discovery of Novel Indazole Derivatives as Orally Available?EBI
Asahi Kasei Pharma
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 DEBI
University of Camerino
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-HTEBI
University of Camerino
Return of DEBI
University of Nebraska Medical Center
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.EBI
American Cyanamid
Discovery of selective, orally bioavailable, N-linked arylsulfonamide NaEBI
Department of Discovery Chemistry Merck
Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.BDB
Case Western Reserve University
(Phenylpiperazinyl)cyclohexylureas: discovery of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).BDB
Johnson & Johnson Pharmaceutical Research and Development
Differential effects of the 5-hydroxytryptamine (5-HT)1A receptor inverse agonists Rec 27/0224 and Rec 27/0074 on electrophysiological responses to 5-HT1A receptor activation in rat dorsal raphe nucleus and hippocampus in vitro.BDB
Universit&Aagrove
S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.BDB
Institut De Recherches Servier
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.BDB
Institut De Recherches Servier
Biochemistry and pharmacology of epitope-tagged alpha(1)-adrenergic receptor subtypes.BDB
Emory University
Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties.BDB
Abbott Laboratories
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract.BDB
Recordati
Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization.BDB
Institut De Recherches Servier
S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine.BDB
Centre De Recherches De Croissy
Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.BDB
Institut De Recherches Servier