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141 articles for thisTarget


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

PMID
Data
Article Title
Organization
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.EBI
Jagiellonian University Medical College
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.EBI
Merck Research Laboratories
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
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-actingß2-adrenoceptor agonist.EBI
Novartis Institutes For Biomedical Research
Discovery of TD-4306, a long-actingß2-agonist for the treatment of asthma and COPD.EBI
Theravance
Multivalent design of long-actingß(2)-adrenoceptor agonists incorporating biarylamines.EBI
Theravance
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.EBI
Glaxosmithkline
Synthesis and in vitro and in vivo characterization of highlyß1-selectiveß-adrenoceptor partial agonists.EBI
University Of Nottingham
Structure-based fragment screening is demonstrated to be a practical lead discovery method for a representative G-protein-coupled receptor.EBI
Pfizer
Biophysical fragment screening of theß1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.EBI
Heptares Therapeutics
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for humanß-adrenoceptors.EBI
University Of Nottingham
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.EBI
Novartis Institutes For Biomedical Research
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.EBI
Glaxosmithkline
An investigation into the structure-activity relationships associated with the systematic modification of theß(2)-adrenoceptor agonist indacaterol.EBI
Novartis Institutes For Biomedical Research
From libraries to candidate: the discovery of new ultra long-acting dibasicß2-adrenoceptor agonists.EBI
Astrazeneca
A multivalent approach to the discovery of long-actingß(2)-adrenoceptor agonists for the treatment of asthma and COPD.EBI
Theravance
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating a urea group.EBI
Glaxosmithkline
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating hydantoin or uracil rings.EBI
Glaxosmithkline
Design-driven LO: the discovery of new ultra long acting dibasicß2-adrenoceptor agonists.EBI
Astrazeneca
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.EBI
Glaxosmithkline
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.EBI
Glaxosmithkline
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.EBI
Smithkline Beecham Pharmaceuticals
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.EBI
H. Lundbeck
Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents.EBI
Sk Biopharmaceuticals
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
Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.EBI
TBA
Synthesis and Cardiac Imaging of (18)F-Ligands Selective for ß1-Adrenoreceptors.EBI
TBA
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.EBI
University Of Namur
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 {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relaEBI
Pfizer
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.EBI
Aska Pharmaceutical
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
Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.EBI
Merck Research Laboratories
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
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the beta2-adrenergic receptor: part 6.EBI
Astellas Pharma
Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.EBI
Astellas Pharma
Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.EBI
Astellas Pharma
Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety.EBI
Astellas Pharma
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.EBI
Tom'S Of Maine
Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I.EBI
Astellas Pharma
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.EBI
Pfizer
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI
Novartis Institutes For Biomedical Research
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.EBI
Fujisawa Pharmaceutical
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.EBI
Pfizer
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).EBI
Purdue University
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.EBI
Wyeth-Ayerst Research
From hit to lead. Analyzing structure-profile relationships.EBI
Universities Of Lille
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).EBI
Abbott Laboratories
Synthesis and pharmacological studies of N-[4-[2-hydroxy-3-[[2-[4-(1H-imidazol-1- yl)phenoxy]ethyl]amino]propoxy]phenyl]methanesulfonamide, a novel antiarrhythmic agent with class II and class III activities.EBI
Berlex Laboratories
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.EBI
Berlex Laboratories
Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene.EBI
TBA
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI
Virginia Commonwealth University
Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-ß2-agonist for the treatment of chronic obstructive pulmonary disease.EBI
Pfizer
Synthesis and in vitro evaluation of derivatives of theß¿?-adrenergic receptor antagonist HX-CH 44.EBI
University Of Toronto
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.EBI
Medical University Of Lublin
Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective humanß3 adrenergic receptor agonists.EBI
Merck Research Laboratories
Thienopyrimidines asß3-adrenoceptor agonists: hit-to-lead optimization.EBI
4Sc
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical And Public Health Institute
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.EBI
Novartis Institutes For Biomedical Research
Identification of potent and selective amidobipyridyl inhibitors of protein kinase D.EBI
Novartis Institutes For Biomedical Research
Identification of orally available naphthyridine protein kinase D inhibitors.EBI
Novartis Institutes For Biomedical Research
Smoothened antagonists for hair inhibition.EBI
Pfizer
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI
Università
A vHTS approach for the identification of beta-adrenoceptor ligands.EBI
4Sc
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.EBI
Meiji Seika Kaisha
Discovery of olodaterol, a novel inhaled beta2-adrenoceptor agonist with a 24 h bronchodilatory efficacy.EBI
Boehringer Ingelheim Pharma
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI
University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj
Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action.EBI
Boehringer Ingelheim Pharma
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as beta2-adrenoceptor agonists.EBI
Boehringer Ingelheim Pharma
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.EBI
Novartis Institutes For Biomedical Research
 
Carboxyl-promoted enhancement of selectivity for the β3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-β3 binding selectivityEBI
TBA
 
BMS-187257, a potent, selective, and novel heterocyclic β3 adrenergic receptor agonistEBI
TBA
Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.EBI
Glaxosmithkline
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5.EBI
Astellas Pharma
Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists.EBI
Astellas Pharma
Substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes as beta3-adrenergic receptor agonists: design, synthesis, biological evaluation and pharmacophore modeling.EBI
Central Drug Research Institute
Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV.EBI
Astellas Pharma
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI
Merck Research Laboratories
Facile radiosynthesis of fluorine-18 labeled beta-blockers. Synthesis, radiolabeling, and ex vivo biodistribution of [18F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol.EBI
Centre For Addiction And Mental Health
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI
Amgen
Discovery of a novel series of biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II.EBI
Astellas Pharma
Potent oxindole based human beta3 adrenergic receptor agonists.EBI
Eli Lilly
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.EBI
Eli Lilly
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.EBI
Pfizer
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.EBI
National Institute Of Mental Health
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
Glaxosmithkline
Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.EBI
Università
Potent benzimidazolone based human beta(3)-adrenergic receptor agonists.EBI
Eli Lilly
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.EBI
Predix Pharmaceuticals
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
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.EBI
F. Hoffmann-La Roche
Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.EBI
Dainippon Pharmaceutical
Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.EBI
Dainippon Pharmaceutical
Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.EBI
Dainippon Pharmaceutical
Binding of beta-carbolines at 5-HT(2) serotonin receptors.EBI
Virginia Commonwealth University
Cyclic amine sulfonamides as linkers in the design and synthesis of novel human beta(3) adrenergic receptor agonists.EBI
Wyeth Research
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.EBI
Dainippon Pharmaceutical
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.EBI
Universita Di Camerino
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines.EBI
Wyeth Research
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.EBI
Wyeth Research
4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor.EBI
Wyeth-Ayerst Research
New oxadiazolidinedione derivatives as potent and selective human beta3 agonists.EBI
Wyeth-Ayerst Research
2,4-Thiazolidinediones as potent and selective human beta3 agonists.EBI
Wyeth-Ayerst Research
Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.EBI
Merck Research Laboratories
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.EBI
Merck Research Laboratories
Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.EBI
Merck Research Laboratories
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.EBI
Merck Research Laboratories
Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.EBI
Merck Research Laboratories
Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.EBI
Merck Research Laboratories
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.EBI
Merck Research Laboratories
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.EBI
Merck Research Laboratories
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.EBI
Merck Research Laboratories
S1319: a novel beta2-andrenoceptor agonist from a marine sponge Dysidea sp.EBI
Kirin Brewery
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.EBI
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.EBI
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.EBI
Merck Research Laboratories
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.EBI
Merck Research Laboratories
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.EBI
Merck Research Laboratories
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.EBI
Merck Research Laboratories
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.EBI
Merck Research Laboratories
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
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.EBI
Università
Synthesis, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents.EBI
Berlex Laboratories
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.BDB
Yogi Vemana University
Deazaflavin Inhibitors of Tyrosyl-DNA Phosphodiesterase 2 (TDP2) Specific for the Human Enzyme and Active against Cellular TDP2.BDB
National Institutes Of Health
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University Of Leipzig
Amplification of the rat M2 muscarinic receptor gene by the polymerase chain reaction: functional expression of the M2 muscarinic receptor.BDB
University Of Arizona