92 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
Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases.
Universit?? Degli Studi Di Siena
Defining the communication between agonist and coactivator binding in the retinoid X receptor a ligand binding domain.
University Of Alabama At Birmingham
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
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.
University Of Leipzig
Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides.
Dupont Pharmaceuticals
In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.
Smithkline Beecham Pharmaceuticals
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Abbott Laboratories