5-hydroxytryptamine uptake blockers attenuate the 5-hydroxytryptamine-releasing effect of 3,4-methylenedioxymethamphetamine and related agents.
C. R. Hekmatpanah, S. Peroutka
European Journal of Pharmacology February 20, 1990 DOI: 10.1016/0014-2999(90)90555-k (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Peer reviewed |
|---|---|
| Population | Rat brain synaptosomes |
| Interventions | 3 4-methylenedioxymethamphetamine (MDMA) 5-HT uptake blockers |
| Measures | [3H]5-HT release, EC50, [3H]paroxetine binding affinity |
| Topics | MDMA |
| Key points | MDMA and related agents release [3H]5-HT from rat brain synaptosomes, and serotonin uptake blockers dose-dependently block this release. The blocking potencies of these drugs correlate strongly with their affinity for the [3H]paroxetine-labeled serotonin uptake site (r = 0.98), indicating the serotonin uptake carrier is significantly involved in MDMA-induced serotonin release. |
Abstract
This study examined the [3H]5-HT-releasing properties of 3,4-methylenedioxymethamphetamine (MDMA) and related agents, all of which cause significant release of [3H]5-HT from rat brain synaptosomes. 5-HT uptake blockers dose dependently block MDMA-induced [3H]5-HT release. The EC50s of the uptake drugs in blocking MDMA-induced release correlate with their affinity for the 5-HT uptake site labeled by [3H]paroxetine (r = 0.98; P less than 0.01). These data demonstrate that the 5-HT uptake carrier plays a significant role in the release of 5-HT induced by MDMA and related agents.