Abstract
We have tested the ability of (±)-CP 96,345, a novel nonpeptide substance P (SP) antagonist, to block the aversive behaviour induced by intrathecal (i.t.) administration of SP and to induce thermal antinociception in mice. (±)-CP 96,345 administered i.t. or i.p. selectively blocked the effect of i.t. SP while leaving the response to i.t. bombesin unaffected. At the same dose proven effective against i.t. SP, (±)-CP 96,345 produced thermal analgesia in the hot plate test (52°C). Using isolated organs for bioassay evaluation of activity at tachykinin receptor, (±)-CP 96,345 was found to be a potent (pA 2 8.11, c.l. 7.9–8.3) and competitive NK 1 receptor antagonist while it was devoid of activity at NK 2 or NK 3 receptors. These findings provide clear indication for the participation of SP, via NK 1 receptors, in thermal nociception.
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