Abstract

(+)-(2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine (CP-99,994) binds with high affinity (pK i 9.6) to the human NK 1 receptor. Racemic analogues of CP-99,994 containing either benzoyl or diazirinyl moieties also bind with high affinity (pK i 9.4 and 9.1 respectively). These analogues are of tremendous potential for mapping the antagonist binding site of the NK 1 receptor.

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