PMID

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Article Title

Organization

Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues.

Sankyo

Cyclic peptides as selective tachykinin antagonists.

Merck Sharp and Dohme Research Laboratories

 

Peptide azoles: A new class of biologically-active dipeptide mmetics.

TBA

2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.

Novartis Institute For Medical Sciences

Studies on neurokinin antagonists. 4. Synthesis and structure-activity relationships of novel dipeptide substance P antagonists: N2-[(4R)-4-hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl]-N- methyl-N-(phenylmethyl)-3-(2-naphthyl)-L-alaninamide and its related compounds.

Fujisawa Pharmaceutical

Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand.

Pfizer

Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.

Glaxo Group Research

Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists.

Fujisawa Pharmaceutical

Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.

The Schering Plough Research Institute

Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.

Novartis Institute For Medical Sciences

Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.

Yamanouchi Pharmaceutical

 

Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity

TBA

 

An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345.

TBA

 

Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H₁/NK₁ receptor antagonist activity

TBA

 

Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK₁/NK₂ receptor antagonists

TBA

 

Perhydrothiopyranopyrroles derivatives : A novel series of potent and selective nonpeptide NK1 antagonists.

TBA

 

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

TBA

 

Methionine replacements in biologically active peptides

TBA

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

Sankyo

Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P.

Hebrew University of Jerusalem

3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.

Eli Lilly

Studies on neurokinin antagonists. 3. Design and structure-activity relationships of new branched tripeptides N alpha-(substituted L-aspartyl, L-ornithyl, or L-lysyl)-N-methyl-N-(phenylmethyl)-L-phenylalaninamides as substance P antagonists.

Fujisawa Pharmaceutical

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

Glaxo Wellcome Medicines Research Centre

[pGlu6,Pro9]SP6-11, a selective agonist for the substance P P-receptor subtype.

TBA

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

Hebrew University of Jerusalem

Potent and highly selective neurokinin antagonists.

Glaxo Group Research