93 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Glaxosmithkline
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
Development of novel NK3 receptor antagonists with reduced environmental impact.
Kyoto 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
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).
Euroscreen
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
Euroscreen
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
Kyoto University
Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.
Universit£
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Merck Research Laboratories
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
Universit£
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Bristol-Myers Squibb
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
Kyoto University
3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor.
Northeast Ohio Medical University
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.
Glaxosmithkline
New quinoline NK3 receptor antagonists with CNS activity.
Neuroscience Cedd Glaxosmithkline Research & Development
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonists.
F. Hoffmann-La Roche
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.
Aska Pharmaceutical
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.
Merck Sharp & Dohme Research Laboratories
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
Astrazeneca Pharmaceuticals
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).
Smithkline Beecham
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
Cambridge University Forvie Site
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.
Smithkline Beecham
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
Merck Sharp Laboratory
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds
TBA
The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists
TBA
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design
TBA
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.
Euroscreen
Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists.
Astrazeneca Pharmaceuticals
Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.
Northeastern Ohio Universities Colleges of Medicine and Pharmacy
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.
F. Hoffmann-La Roche
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.
F. Hoffmann-La Roche
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.
F. Hoffmann-La Roche
SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist
TBA
The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanes
TBA
Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening.
TBA
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Merck Research Laboratories
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
Schering-Plough Research Institute
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Merck
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.
Merck Sharp & Dohme Research Laboratories
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Merck Research Laboratories
Cyclobutane derivatives as potent NK1 selective antagonists.
Schering-Plough Research Institute
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.
Astrazeneca Pharmaceuticals
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.
Schering-Plough Research Institute
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Pharmazeutisches Institut Der UniversitäT Freiburg
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.
Smithkline Beecham Pharmaceuticals
Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact.
Kyoto University
High affinity phenylglycinol-based NK1 receptor antagonists.
Merck Sharp and Dohme Research Laboratories
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.
Smithkline Beecham S.P.A. Milano
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
China Pharmaceutical University
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Merck Research Laboratories
Comparison of the conformation of active and nonactive backbone cyclic analogs of substance P as a tool to elucidate features of the bioactive conformation: NMR and molecular dynamics in DMSO and water.
Technische UniversitäT MüNchen
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
Merck Sharp and Dohme Research Laboratories
Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.
Menarini Ricerche
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
Sanofi-Synthelabo Recherche
SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization.
Sanofi-SynthÉLabo Recherche
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.
Schering-Plough Research Institute
Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.
Glaxosmithkline
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
Novartis Pharma
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Janssen Research Foundation
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Sanofi Recherche
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Smithkline Beecham Pharmaceuticals
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.
Abbott Laboratories
SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.
Sanofi Recherche