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Updated: Jul 19, 2026
09:16
A General Method for Evaluating Deep Brain Stimulation Effects on Intravenous Methamphetamine Self-Administration
Published on: January 22, 2016
Interactions between 3,4-methylenedioxymethamphetamine and sigma1 receptors.
Matthew K Brammer1, Deborah L Gilmore, Rae R Matsumoto
1Department of Pharmaceutical Sciences, College of Pharmacy, University of Oklahoma Health Sciences Center, Oklahoma City, OK, 73190 USA.
European Journal of Pharmacology
|October 31, 2006
Summary
3,4-methylenedioxymethamphetamine (MDMA) interacts with sigma(1) receptors, influencing its stimulant effects. Blocking these sigma(1) receptors with BD1063 attenuated MDMA-induced hyperactivity in mice, supporting a role for sigma(1) in MDMA
Area of Science:
- Neuroscience
- Pharmacology
- Toxicology
Background:
- Methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA) are structurally related stimulants with significant health implications.
- Previous research indicated methamphetamine's interaction with sigma receptors, suggesting a potential therapeutic target for its adverse effects.
- The specific interaction between MDMA and sigma receptors remained uncharacterized.
Purpose of the Study:
- To investigate the involvement of sigma receptors in the pharmacological actions of MDMA.
- To determine if MDMA binds to sigma receptors and to identify the specific subtype involved.
- To assess the behavioral effects of blocking sigma(1) receptors on MDMA-induced stimulation.
Main Methods:
- Competition and saturation binding assays were employed to quantify MDMA's affinity for sigma(1) and sigma(2) receptors.
- Locomotor activity in male Swiss Webster mice was measured following administration of MDMA and a selective sigma(1) receptor antagonist, BD1063.
- Dose-response curves were analyzed to evaluate the effects of BD1063 on MDMA-induced hyperactivity.
Main Results:
- MDMA demonstrated a preferential and competitive binding interaction with the sigma(1) receptor subtype over the sigma(2) subtype.
- The sigma(1) receptor antagonist BD1063, administered alone, did not affect locomotor activity.
- BD1063 dose-dependently attenuated the locomotor stimulant effects of MDMA, shifting the dose-response curve significantly.
Conclusions:
- The findings confirm the functional relevance of MDMA's interaction with sigma(1) receptors.
- Sigma(1) receptors play a significant role in mediating the stimulant properties of MDMA.
- Targeting sigma(1) receptors may offer a potential strategy for managing MDMA-induced effects.
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