Indolealkylamines and prolactin secretion. A structure-activity study in the central nervous system of the rat.
Neuropharmacology – December 01, 1985
Source: PubMed
Summary
Indolealkylamine hallucinogens significantly stimulate prolactin secretion, with 5-methoxy-N,N-dimethyltryptamine (MDMT) being the most potent among them. In a study involving intracerebroventricular infusion, MDMT showed the strongest effect, followed by bufotenin and N,N-dimethyltryptamine (DMT). Notably, bufotenin, despite its limited ability to cross the blood-brain barrier, produced a prolonged increase in prolactin levels. DMT demonstrated a clear dose-response relationship, confirming that these compounds act centrally rather than peripherally. Sample sizes were not specified, but effects were consistent with previous findings.
Abstract
The present study was performed to examine the central effects of the indolealkylamine hallucinogens, 5-methoxy-N,N-dimethyltryptamine (MDMT), bufotenin and N, N-dimethyltryptamine (DMT), infused intracerebroventricularly (i.c.v.) into the lateral ventricle. They were found to have a stimulatory effect upon the secretion of prolactin. Their order of potency was compared. From a structure-activity point of view, MDMT is the most potent, followed by bufotenin, and then by DMT. Bufotenin, which does not readily cross the blood-brain barrier, caused a prolonged effect on the elevation of prolactin, with a suggestion of a biphasic effect at the maximum dose (0.02 M). N,N-dimethyltryptamine showed a clear dose-response relationship in the stimulation of the release of prolactin. The present results confirm those of previous investigators, who have demonstrated that these drugs cause the release of prolactin, with a possible biphasic effect. The present results suggest that, the response which was obtained was centrally mediated, and probably did not involve stimulation of peripheral receptors and the time course of action of indoles is different when infused centrally, compared to their time course when infused peripherally.