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

Journal Article · Fri Jan 25 04:00:00 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), Journal Name: Science (Washington, D.C.); (United States) Vol. 251:4992; ISSN SCIEA; ISSN 0036-8075
• Country of Publication: United States
• Language: English

Related Subjects

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