A potent nonpeptide antagonist of the substance P (NK sub 1 ) receptor

Journal Article · Fri Jan 25 00:00:00 EST 1991 · Science (Washington, D.C.); (United States)

DOI:https://doi.org/10.1126/science.1703323· OSTI ID:5821865

Snider, R M; Constantine, J W; Lowe, III, J A; Longo, K P; Lebel, W S; Woody, H A; Drozda, S E; Desai, M C; Vinick, F J; Spencer, R W; Hess, H J ^[1]

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1. Pfizer Inc., Groton, CT (United States)

CP-96,345 ((2S, 3S)-cis-2-(diphenylmethyl)-N-((2-methoxyphenyl)-methyl)-1-azabicyclo(2.2.2)octan-3-amine) is a potent nonpeptide antagonist of the substance P (NK{sub 1}) receptor. CP-96,345 inhibited {sup 3}H-labeled substance P binding and was a classical competitive antagonist in the NK{sub 1} monoreceptor dog carotid artery preparation. CP-96,345 inhibited substance P-induced salivation in the rat, a classical in vivo bioassay, but did not inhibit NK{sub 2}, NK{sub 3}, or numerous other receptors; it is thus a selective NK{sub 1} antagonist. This compound may prove to be a powerful tool for investigation of the physiological properties of substance P and exploration of its role in diseases.

• OSTI ID: 5821865
• Journal Information: Science (Washington, D.C.); (United States), Vol. 251:4992; ISSN 0036-8075
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
KININS
RECEPTORS
LIGANDS
BIOCHEMICAL REACTION KINETICS
CAROTID ARTERIES
DOGS
INHIBITION
RATS
SALIVARY GLANDS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
ARTERIES
BLOOD VESSELS
BODY
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HYDROGEN COMPOUNDS
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MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANS
PEPTIDES
POLYPEPTIDES
PROTEINS
REACTION KINETICS
RODENTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques