Effect of CP-96,345, a nonpeptide substance P receptor antagonist, on salivation in rats.

Authors :: Snider, R M
Longo, K P
Drozda, S E
Lowe, J A
Leeman, S E
Source :: Proceedings of the National Academy of Sciences of the United States of America; November 1991, Vol. 88 Issue: 22 p10042-10044, 3p
Publication Year :: 1991
Abstract: CP-96,345 [(2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl) methyl]-1-azabicyclo[2.2.2]octan-3-amine) antagonism of substance P-stimulated salivation was investigated in pentobarbital-anesthetized rats. Administered either intraperitoneally or orally, CP-96,345 produced dose-dependent inhibition of the sialogogic response elicited by substance P, with a median effective dose of 12-24 mumol/kg (5-10 mg/kg) of body weight, but had no effect on acetylcholine-stimulated salivation. CP-96,345 produced concentration-dependent inhibition of [3H]substance P binding to rat submaxillary gland membranes, with a median effective concentration of 34 +/- 3.6 nM. These biological activities were confined to CP-96,345 in that the 2R,3R enantiomer (CP-96,344) was without effect.

Language :: English
ISSN :: 00278424 and 10916490
Volume :: 88
Issue :: 22
Database :: Supplemental Index
Journal :: Proceedings of the National Academy of Sciences of the United States of America
Publication Type :: Periodical
Accession number :: ejs60450095
Full Text :: https://doi.org/10.1073/pnas.88.22.10042

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