Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist.

Science (New York, N.Y.) ·Vol. 251 ·No. 4992 ·1991-01-25 ·Pages 437-9

McLean S, Ganong AH, Seeger TF, Bryce DK, Pratt KG, Reynolds LS, Siok CJ, Lowe JA, Heym J

Abstract

CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK1 receptor. The compound binds to a single population of sites in guinea pig brain and potently inhibits substance P-induced excitation of locus ceruleus neurons. CP-96,345 should be a useful tool for studying the action of substance P in the central nervous system.

MeSH Terms

Action Potentials Animals Autoradiography Binding Sites Binding, Competitive Biphenyl Compounds/metabolism,pharmacology Brain/diagnostic imaging,metabolism Corpus Striatum/diagnostic imaging,metabolism Guinea Pigs Hydrogen-Ion Concentration Male Radionuclide Imaging Receptors, Neurokinin-1 Receptors, Neurotransmitter/antagonists & inhibitors,metabolism Receptors, Tachykinin Spectrophotometry Substance P/metabolism Tachykinins/metabolism

Chemicals

Biphenyl Compounds Receptors, Neurokinin-1 Receptors, Neurotransmitter Receptors, Tachykinin Tachykinins Substance P CP 96345

Authors & Affiliations

9 authors, click to expand affiliations / ORCID

McLean S

Department of Neuroscience, Central Research Division, Pfizer Inc., Groton, CT 06340.

Ganong A H

Seeger T F

Bryce D K

Pratt K G

Reynolds L S

Siok C J

Lowe J A

Heym J

Article Info

Journal

Science (New York, N.Y.)

Abbr.

Science

ISSN

0036-8075

DOI

10.1126/science.1703324

Published

1991-01-25

Pages

437-9

Language

English

Region

United States

NLM ID

0404511

Subset

External Links

PubMed source DOI: 10.1126/science.1703324 View journal details

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Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist.

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