Effects of the selective 5-HT2A receptor antagonist
MDL 100,907 on MDMA-induced locomotor stimulation in rats

by
Kehne JH, Ketteler HJ, McCloskey TC,
Sullivan CK, Dudley MW, Schmidt CJ.
Hoechst Marion Roussel, Inc.,
Cincinnati, OH 45215, USA.
Neuropsychopharmacology 1996 Aug;15(2):116-24


ABSTRACT

(+/-)3,4-Methylenedioxymethamphetamine (MDMA) releases dopamine and serotonin in vivo and stimulates locomotor activity. Previous work demonstrated that MDMA-stimulated dopamine release could be reduced by the selective 5-HT2A receptor antagonist [R-(+)-a- (2,3-dimethoxyphenyl)-1-[2-(4-fluorophenylethyl)]-4-piperidinem ethanol] (MDL 100,907). In the present study MDL 100,907 significantly reduced MDMA-stimulated locomotion without affecting basal levels of locomotion. Other agents with 5-HT2A antagonist activity (ritanserin, clozapine, MDL 28,133A, or methiothepin), as well as agents that block 5-HT1A-(propranolol), D2-(haloperidol), or D1 receptors (SCH 23390) also reduced MDMA-stimulated locomotion. Intraventricularly administered 5,7-dihydroxytryptamine decreased regional 5-HT levels and attenuated MDMA-stimulated locomotion. These data support the conclusion that serotonin released onto 5-HT2A receptors contributes to MDMA-stimulated locomotion and suggest that MDMA-stimulated locomotion may be useful as an in vivo behavioral measure of 5-HT2A antagonism. The data also support previous reports of contributions of 5-HT1A, D1 and D2 receptors to MDMA-stimulated locomotion. A preliminary time-course analysis indicating time-dependent contributions of different receptors to MDMA-stimulated locomotion suggests the potential utility of this model for characterizing potential atypical antipsychotic compounds.

History
Attention
MDMA/MDE
Controversies
Oxidative stress
MDMA v fenfluramine
Baboons like Ecstasy
Cutaneous vasoconstriction
Ecstasy/MDMA and cannabis
Arginine-vasopressin release
MDMA, loud noise and the heart
MDMA, HIV and antiretroviral agents
Serotonin, noradrenline and dopamine
MDMA/polydrug users in the UK and Italy
Ecstasy (MDMA), locomotion and the nucleus accumbens


Refs
and further reading

HOME
HedWeb
Nootropics
cocaine.wiki
Future Opioids
BLTC Research
MDMA/Ecstasy
Superhapiness?
Utopian Surgery?
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World

The Good Drug Guide
The Good Drug Guide

The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family