Description:
<jats:p>
CP-96,345 [(2
<jats:italic>S</jats:italic>
, 3
<jats:italic>S</jats:italic>
)-
<jats:italic>cis</jats:italic>
-2-(diphenylmethyl)-
<jats:italic>N</jats:italic>
-[(2-methoxyphenyl)-methyl]-1-azabicyclo[2.2.2]octan-3-amine] is a potent nonpeptide antagonist of the substance P (NK
<jats:sub>1</jats:sub>
) receptor. CP-96,345 inhibited
<jats:sup>3</jats:sup>
H-labeled substance P binding and was a classical competitive antagonist in the NK
<jats:sub>1</jats:sub>
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
<jats:sub>2</jats:sub>
, NK
<jats:sub>3</jats:sub>
, or numerous other receptors; it is thus a selective NK
<jats:sub>1</jats:sub>
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.
</jats:p>