SR-142801, THE FIRST POTENT NONPEPTIDE ANTAGONIST OF THE TACHYKININ NK3 RECEPTOR

Authors
EMONDSALT X BICHON D DUCOUX JP HEAULME M MILOUX B PONCELET M PROIETTO V VANBROECK D VILAIN P NELIAT G SOUBRIE P LEFUR G BRELIERE JC
Citation
X. Emondsalt et al., SR-142801, THE FIRST POTENT NONPEPTIDE ANTAGONIST OF THE TACHYKININ NK3 RECEPTOR, Life sciences, 56(1), 1994, pp. 161200027-161200032
Citations number
16
Categorie Soggetti
Biology,"Medicine, Research & Experimental","Pharmacology & Pharmacy
Journal title
Life sciences → ACNP
ISSN journal
00243205
Volume
56
Issue
1
Year of publication
1994
Pages
161200027 - 161200032
Database
ISI
SICI code
0024-3205(1994)56:1<161200027:STFPNA>2.0.ZU;2-0
Abstract
SR 142801 is the first potent and selective non-peptide antagonist of the tachykinin NK3 receptor. It inhibited [MePhe(7)]NKB binding to its receptor from various species, including humans. SR 142801 was a comp etitive antagonist of [MePhe(7)]NKB-mediated contractions of guinea-pi g ileum and inhibited the acetylcholine release following the activati on of the guinea-pig ileum tachykinin NK3 receptor. In vivo, SR 142801 potently inhibited the turning behaviour induced by intrastriatal inj ection of senktide in gerbils, and appears as a powerful tool for inve stigation of the physiological and pathological role of NKB and its NK 3 receptor.