A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor

X Emonds-Alt; P Vilain; P Goulaouic; V Proietto; D Van Broeck; C Advenier; E Naline; G Neliat; G Le Fur; J C Brelière

doi:10.1016/0024-3205(92)90352-p

A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor

Life Sci. 1992;50(15):PL101-6. doi: 10.1016/0024-3205(92)90352-p.

Authors

X Emonds-Alt¹, P Vilain, P Goulaouic, V Proietto, D Van Broeck, C Advenier, E Naline, G Neliat, G Le Fur, J C Brelière

Affiliation

¹ Sanofi Recherche, Montpellier, France.

PMID: 1313515
DOI: 10.1016/0024-3205(92)90352-p

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.

MeSH terms

Animals
Benzamides / chemistry
Benzamides / pharmacology*
Binding, Competitive
Bronchoconstriction / drug effects
Cricetinae
Duodenum / metabolism
Intestinal Mucosa / metabolism
Neurokinin A / antagonists & inhibitors*
Piperidines*
Rabbits
Rats
Receptors, Neurokinin-2
Receptors, Neurotransmitter / drug effects*
Vasoconstriction / drug effects

Substances

Benzamides
Piperidines
Receptors, Neurokinin-2
Receptors, Neurotransmitter
SR 48968
Neurokinin A