PMID

Data

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£

Design and synthesis of potential dual NK(1)/NK(3) 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

Discovery of novel, orally active dual NK1/NK2 antagonists.

Astrazeneca Pharmaceuticals

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

 

2,3-Substituted 2-azanorbornanes as polar -turn mimetics

TBA

 

The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists

TBA

 

The design of polar -turn dipeptide mimetics

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

Identification of a new series of non-peptidic NK3 receptor antagonists.

H. Lundbeck

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

 

A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist

TBA

 

Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK₁ and NK₂ receptors

TBA

 

The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptors

TBA

 

SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK₁ antagonist

TBA

 

Piperidine-ether based hNK₁ antagonists 2: Investigation of the effect of N-substitution

TBA

 

Alternative strategies towards the identification of chemical lead compounds by rational design

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

 

Methionine replacements in biologically active peptides

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

Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.

Sankyo

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

New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists.

Glaxo Wellcome Medicines Research Centre

Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.

Phenex Pharmaceuticals

Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity.

Hebrew University Of Jerusalem

The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.

Pfizer

Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.

Columbia University

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

N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.

Pudue Pharma Discovery Research

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

Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.

Eli Lilly

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

Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.

Eli Lilly

The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.

Janssen Research Foundation

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories

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

In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist.

Hoechst Marion Roussel

GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.

Glaxo Group Research

SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.

Sanofi Recherche

Functional characterization of the nonpeptide neurokinin3 (NK3) receptor antagonist, SR142801 on the human NK3 receptor expressed in Chinese hamster ovary cells.

Sanofi Recherche