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

Life sciences ·Vol. 50 ·No. 15 ·1992-00-00 ·Pages PL101-6

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

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,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

Chemicals

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

Authors & Affiliations

10 authors, click to expand affiliations / ORCID

Emonds-Alt X

Sanofi Recherche, Montpellier, France.

Vilain P

Goulaouic P

Proietto V

Van Broeck D

Advenier C

Naline E

Neliat G

Le Fur G

Brelière J C

Article Info

Journal

Life sciences

Abbr.

Life Sci

ISSN

0024-3205

DOI

10.1016/0024-3205(92)90352-p

Published

1992-00-00

Pages

PL101-6

Language

English

Region

Netherlands

NLM ID

0375521

Subset

External Links

PubMed source DOI: 10.1016/0024-3205(92)90352-p View journal details

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

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