Activity and Distribution of Binding Sites in Brain of a Nonpeptide Substance P (NK$_1$) Receptor Antagonist

CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK$_1$ 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 a...

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Veröffentlicht in:Science (American Association for the Advancement of Science) 1991-01, Vol.251 (4992), p.437-439
Hauptverfasser: McLean, Stafford, Ganong, Alan H., Seeger, Thomas F., Bryce, Dianne K., Pratt, Kara G., Reynolds, Linda S., Siok, Chester J., Lowe, John A., Heym, James
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Sprache:eng
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Zusammenfassung:CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK$_1$ 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.
ISSN:0036-8075
1095-9203
DOI:10.1126/science.1703324