A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor.
SR 48968 is a potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor. SR 48968 selectively inhibited neurokinin A binding to its receptor and was a competitive antagonist of neurokinin A-mediated contraction of different isolated smooth muscle preparations from various species including human. In vivo, the compound inhibited the bronchoconstriction induced by neurokinin A in guinea pigs. SR 48968 can be used to study the physiological or pathological role of neurokinin A and may be useful in the treatment of neurokinin A-dependent pathology.
Emonds-Alt
X
X
Sanofi Recherche, Montpellier, France.
Vilain
P
P
Goulaouic
P
P
Proietto
V
V
Van Broeck
D
D
Advenier
C
C
Naline
E
E
Neliat
G
G
Le Fur
G
G
Brelière
J C
JC
D000818:Animals; D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology*; D001667:Binding, Competitive; D016084:Bronchoconstriction / Q000187:drug effects; D006224:Cricetinae; D004386:Duodenum / Q000378:metabolism; D007413:Intestinal Mucosa / Q000378:metabolism; D015288:Neurokinin A / Q000037:antagonists & inhibitors*; D010880:Piperidines; D011817:Rabbits; D051381:Rats; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter / Q000187:drug effects*; D014661:Vasoconstriction / Q000187:drug effects
D001549:Benzamides; D010880:Piperidines; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter; C073839:SR 48968; D015288:Neurokinin A