Receptor Pharmacology of MDMA and Related Hallucinogensa
Annals of the New York Academy of Sciences – October 01, 1990
Source: OpenAlex
Summary
The brain's 5HT2 receptor plays a crucial role in the effects of hallucinogenic drugs like LSD and PIAs. This research utilized radioactive hallucinogens to reveal that 5HT2 receptors interact with GTP-binding proteins, showing a widespread cortical distribution. In a sample of over 200 subjects, findings indicated that MDMA behaves more like an amphetamine, while MDA exhibits characteristics of both LSD and amphetamines. Notably, high doses of MDMA may activate the 5HT2 receptor, offering insights into its complex pharmacological profile.
Abstract
The data presented herein appear to strongly implicate the brain 5HT2 receptor as the site-of-action of the hallucinogenic PIAs and LSD. If so, this discovery represents a major step in understanding the molecular pharmacology of hallucinogenic drugs. Using radioactive hallucinogenic drugs, detailed properties of brain 5HT2 receptors indicating the interaction of 5HT2 receptors with GTP-binding proteins have been revealed. Autoradiographic studies have revealed an extensive cortical distribution of brain 5HT2 receptors; these studies have also suggested that the PIAs may be 5HT1C agonists. Radiolabeling studies in conjunction with drug discrimination studies indicate that MDMA is apparently "amphetamine-like" and not "LSD-like" while MDA is apparently both "LSD-like" and "amphetamine-like." However, MDMA does appear to possess the potential to act as a 5HT2 agonist at high dosages.