Autoinhibition and desensitization of serotonergic responses in guinea pig ileum.

The present study was undertaken to investigate the autoinhibition and desensitization of 5-hydroxytryptamine (5-HT) using another agonist MK-212 on guinea pig ileum. 5-HT and MK-212 produced dose dependent contractions of guinea pig ileum. The responses to MK-212 were reduced in the presence of 5-HT and vice versa. Neither 5-HT nor MK-212 produced any change in the responses to histamine, acetylcholine or KCl. Increase in Ca++ in bathing fluid reversed the desensitization produced by MK-212 or 5-HT. Our data suggest that 5-HT and MK-212 produce desensitization which is specific for serotonergic receptors and possibly involves Ca++ ions.