190 articles for thisTarget
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Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds.
TBA
6,7-Dichloro-1-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinoline . A structurally novel beta-adrenergic receptor blocking agent.
TBA
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1.
Nippon Roche Research Center
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University Of Kansas
Structure-guided development of dualß2 adrenergic/dopamine D2 receptor agonists.
Friedrich-Alexander University
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
University Of Illinois At Chicago
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Merck Research Laboratories
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
Pfizer
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
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.
City University Of New York
Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist..
Theravance Biopharma
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-actingß2-adrenoceptor agonist.
Novartis Institutes For Biomedical Research
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Novartis Institutes For Biomedical Research
Discovery of TD-4306, a long-actingß2-agonist for the treatment of asthma and COPD.
Theravance
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors.
Pfizer
Multivalent design of long-actingß(2)-adrenoceptor agonists incorporating biarylamines.
Theravance
Discovery of AZD3199, An Inhaled Ultralong Acting?2 Receptor Agonist with Rapid Onset of Action.
Astrazeneca
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
Glaxosmithkline
Synthesis and in vitro and in vivo characterization of highlyß1-selectiveß-adrenoceptor partial agonists.
University Of Nottingham
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for humanß-adrenoceptors.
University Of Nottingham
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.
Glaxosmithkline
An investigation into the structure-activity relationships associated with the systematic modification of theß(2)-adrenoceptor agonist indacaterol.
Novartis Institutes For Biomedical Research
From libraries to candidate: the discovery of new ultra long-acting dibasicß2-adrenoceptor agonists.
Astrazeneca
A multivalent approach to the discovery of long-actingß(2)-adrenoceptor agonists for the treatment of asthma and COPD.
Theravance
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating a urea group.
Glaxosmithkline
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating hydantoin or uracil rings.
Glaxosmithkline
Design-driven LO: the discovery of new ultra long acting dibasicß2-adrenoceptor agonists.
Astrazeneca
Design driven HtL: The discovery and synthesis of new high efficacyß2-agonists.
Astrazeneca
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
Glaxosmithkline
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Glaxosmithkline
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
Glaxosmithkline
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
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.
Smithkline Beecham Pharmaceuticals
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Organon Research And Development Group
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
H. Lundbeck
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
TBA
A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design.
Radboud University Nijmegen Medical Centre
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
Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.
TBA
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
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 rela
Pfizer
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
Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.
Merck Research Laboratories
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College And The Graduate Center Of The City University Of New York
Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues.
Glaxosmithkline
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.
Astellas Pharma
Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist.
Instituto Polit£Cnico Nacional (Ipn)
Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.
Astellas Pharma
Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.
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.
Astellas Pharma
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.
Astellas Pharma
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
Pfizer
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.
Fujisawa Pharmaceutical
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
Novartis Horsham Research Centre
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).
Purdue University
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.
Wyeth-Ayerst Research
Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.
University Of Pennsylvania
(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).
Abbott Laboratories
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.
Berlex Laboratories
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
Cell-based and in-silico studies on the high intrinsic activity of two boron-containing salbutamol derivatives at the humanß2-adrenoceptor.
Instituto Polit£Cnico Nacional (Ipn)
Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-ß2-agonist for the treatment of chronic obstructive pulmonary disease.
Pfizer
Synthesis and in vitro evaluation of derivatives of theß¿?-adrenergic receptor antagonist HX-CH 44.
University Of Toronto
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
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.
Medical University Of Lublin
Progress in structure based drug design for G protein-coupled receptors.
Heptares Therapeutics
Inhalation by design: dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD.
Pfizer
Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective humanß3 adrenergic receptor agonists.
Merck Research Laboratories
Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.
Theravance
Discovery of a Potent and Short−Acting Oral Calcilytic with a Pulsatile Secretion of Parathyroid Hormone
TBA
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical And Public Health Institute
Inhalation by design: novel ultra-long-actingß(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
Pfizer
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
Novartis Institutes For Biomedical Research
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
Novartis Institutes For Biomedical Research
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.
Meiji Seika Kaisha
Discovery of olodaterol, a novel inhaled beta2-adrenoceptor agonist with a 24 h bronchodilatory efficacy.
Boehringer Ingelheim Pharma
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
Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.
Pfizer
Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action.
Boehringer Ingelheim Pharma
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as beta2-adrenoceptor agonists.
Boehringer Ingelheim Pharma
Carboxyl-promoted enhancement of selectivity for the β3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-β3 binding selectivity
TBA
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)
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
Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.
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.
Astellas Pharma
Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists.
Astellas Pharma
Substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes as beta3-adrenergic receptor agonists: design, synthesis, biological evaluation and pharmacophore modeling.
Central Drug Research Institute
Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds.
Lundbeck Research Usa
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.
Centre For Addiction And Mental Health
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.
Glaxosmithkline
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.
Astellas Pharma
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
Theravance
Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains.
St. Jude Children'S Research Hospital
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.
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.
National Institute Of Mental Health
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.
Bristol-Myers Squibb Pharmaceutical Research Institute
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor.
Medical University Of Lublin
Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.
Università
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
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
Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.
Dainippon Pharmaceutical
Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.
Dainippon Pharmaceutical
Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.
Dainippon Pharmaceutical
Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Virginia Commonwealth University
Cyclic amine sulfonamides as linkers in the design and synthesis of novel human beta(3) adrenergic receptor agonists.
Wyeth Research
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.
Dainippon Pharmaceutical
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.
Universita Di Camerino
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines.
Wyeth Research
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.
Wyeth Research
4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor.
Wyeth-Ayerst Research
New oxadiazolidinedione derivatives as potent and selective human beta3 agonists.
Wyeth-Ayerst Research
2,4-Thiazolidinediones as potent and selective human beta3 agonists.
Wyeth-Ayerst Research
Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.
Merck Research Laboratories
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.
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.
Merck Research Laboratories
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.
Merck Research Laboratories
Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.
Merck Research Laboratories
Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.
Merck Research Laboratories
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.
Merck Research Laboratories
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
Merck Research Laboratories
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.
Merck Research Laboratories
S1319: a novel beta2-andrenoceptor agonist from a marine sponge Dysidea sp.
Kirin Brewery
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.
Merck Research Laboratories
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
Merck Research Laboratories
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Merck Research Laboratories
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.
Merck Research Laboratories
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.
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 pr
Abbott Laboratories
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
Universitá
Structural analysis of human KDM5B guides histone demethylase inhibitor development.
University Of Oxford
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.
Yogi Vemana University
Deazaflavin Inhibitors of Tyrosyl-DNA Phosphodiesterase 2 (TDP2) Specific for the Human Enzyme and Active against Cellular TDP2.
National Institutes Of Health
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.
University Of Leipzig
Amplification of the rat M2 muscarinic receptor gene by the polymerase chain reaction: functional expression of the M2 muscarinic receptor.
University Of Arizona
Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor.
Duke University
Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.
Institute Of Genetics And Molecular And Cellular Biology (Igbmc)