title: A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor.
abstract: 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.
authors.affiliation: Sanofi Recherche, Montpellier, France.
authors.forename: X
authors.initials: X
authors.lastname: Emonds-Alt
authors.forename: P
authors.initials: P
authors.lastname: Vilain
authors.forename: P
authors.initials: P
authors.lastname: Goulaouic
authors.forename: V
authors.initials: V
authors.lastname: Proietto
authors.forename: D
authors.initials: D
authors.lastname: Van Broeck
authors.forename: C
authors.initials: C
authors.lastname: Advenier
authors.forename: E
authors.initials: E
authors.lastname: Naline
authors.forename: G
authors.initials: G
authors.lastname: Neliat
authors.forename: G
authors.initials: G
authors.lastname: Le Fur
authors.forename: J C
authors.initials: JC
authors.lastname: Brelière
mesh_terms: 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
chemical_list: D001549:Benzamides; D010880:Piperidines; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter; C073839:SR 48968; D015288:Neurokinin A