SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.
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.
Emonds-Alt
X
X
Sanofi Recherche, Montpellier, France.
Bichon
D
D
Ducoux
J P
JP
Heaulme
M
M
Miloux
B
B
Poncelet
M
M
Proietto
V
V
Van Broeck
D
D
Vilain
P
P
Neliat
G
G
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005849:Gerbillinae; D006168:Guinea Pigs; D066298:In Vitro Techniques; D015287:Neurokinin B / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000378:metabolism; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D018042:Receptors, Neurokinin-3 / Q000037:antagonists & inhibitors*; D014661:Vasoconstriction / Q000187:drug effects
D010880:Piperidines; D018042:Receptors, Neurokinin-3; C080394:neurokinin B, MePhe(7)-; D015287:Neurokinin B; C091554:SR 142801