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Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Two classes of structurally different tachykinin neurokinin3 (NK3) antagonists were used to evaluate species difference in antagonist binding between human and rat NK3 receptors. In competitionExpand
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
The use of a dipeptide library as the source of a micromolar chemical lead compound for the human tachykinin NK3 receptor is described. The screening of a dipeptide library through a cloned human NK3Expand
Rational design of high affinity tachykinin NK1 receptor antagonists.
The rational design of a non-peptide tachykinin NK1 receptor antagonist, [(2-benzofuran)-CH2OCO]-(R)-alpha-MeTrp-(S)-NHCH(CH3)P h (28, PD 154075) is described. Compound 28 has a Ki = 9 and 0.35 nMExpand
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design
Abstract Boc(S)Phe(S)PheNH2 (1c) was identified from the biological screening of an in-house dipeptide chemical library as a micromolar NK3 receptor selective ligand (IC50=1150nM). This leadExpand
Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.
This paper describes the synthesis and physical and biological effects of introducing different substituents at the alpha-position of the tryptophan containing neurokinin-1 receptor antagonistExpand
Generation of unnatural α,α-disubstituted amino acid derivatives from cyclic sulfamidates
Cyclic sulfamidates function as excellent precursors to a variety of unnatural α,α-disubstituted amino acid derivatives by ring opening with a suitable nucleophile. Addition of various nucleophilesExpand
The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists
Abstract In this paper we describe the transformation of a series of modified dipeptide NK3 receptor selective ligands, previously developed from a hit identified from the screening of a dipeptideExpand
'Targeted' molecular diversity: design and development of non-peptide antagonists for cholecystokinin and tachykinin receptors.
A drug design strategy to non-peptide small molecule antagonists of neuropeptides is described that targets the molecular diversity which exists in the 'privileged' data set of the physico-chemicalExpand
Structure-based design in drug discovery--the application of a peptoid drug design strategy for the development of non-peptide neuropeptide receptor ligands.
Over the last decade the increasing availability of metabolically- stable non-peptide antagonists targeted at neuropeptide receptors has led directly to a more thorough understanding of the role ofExpand