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

X Emonds-Alt; D Bichon; J P Ducoux; M Heaulme; B Miloux; M Poncelet; V Proietto; D Van Broeck; P Vilain; G Neliat

doi:10.1016/0024-3205(94)00413-m

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

Life Sci. 1995;56(1):PL27-32. doi: 10.1016/0024-3205(94)00413-m.

Authors

X Emonds-Alt¹, D Bichon, J P Ducoux, M Heaulme, B Miloux, M Poncelet, V Proietto, D Van Broeck, P Vilain, G Neliat, et al.

Affiliation

¹ Sanofi Recherche, Montpellier, France.

PMID: 7830490
DOI: 10.1016/0024-3205(94)00413-m

Abstract

SR 142801 is the first potent and selective non-peptide antagonist of the tachykinin NK3 receptor. It inhibited [MePhe7]NKB binding to its receptor from various species, including humans. SR 142801 was a competitive antagonist of [MePhe7]NKB-mediated contractions of guinea-pig ileum and inhibited the acetylcholine release following the activation of the guinea-pig ileum tachykinin NK3 receptor. In vivo, SR 142801 potently inhibited the turning behaviour induced by intrastriatal injection of senktide in gerbils, and appears as a powerful tool for investigation of the physiological and pathological role of NKB and its NK3 receptor.

MeSH terms

Animals
Behavior, Animal / drug effects
Dose-Response Relationship, Drug
Gerbillinae
Guinea Pigs
In Vitro Techniques
Neurokinin B / analogs & derivatives
Neurokinin B / antagonists & inhibitors
Neurokinin B / metabolism
Piperidines / pharmacology*
Rats
Receptors, Neurokinin-3 / antagonists & inhibitors*
Vasoconstriction / drug effects

Substances

Piperidines
Receptors, Neurokinin-3
neurokinin B, MePhe(7)-
Neurokinin B
SR 142801