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Reneman L,, Endert E, de Bruin K, Lavalaye J, Feenstra MG, de Wolff F, Booij J.
“The acute and chronic effects of MDMA (“Ecstasy”) on cortical 5-HT
2A receptors in rat and human brain”.
Neuropsychopharmacology. 2002;26:387–396,.
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Abstract
While the pre-synaptic effects of 3,4- methylenedioxymethamphetamine (MDMA) on serotonin (5-HT) neurons have been studied extensively, little is known about its effects on post-synaptic 5-HT 2 receptors. Therefore, cortical 5-HT 2A receptor densities and 5-HT concentration were studied in MDMA treated rats (10 mg/kg s.c.). Furthermore, 5-HT 2A post-synaptic receptor densities in the cerebral cortex of recent as well as ex-MDMA users were studied using [ 123 I]R91150 SPECT. In rats we observed a decrease followed by a time-dependent recovery of cortical 5-HT 2A receptor densities, which was strongly and positively associated with the degree of 5-HT depletion. In recent MDMA users, post-synaptic 5-HT 2A receptor densities were significantly lower in all cortical areas studied, while 5-HT 2A receptor densities were significantly higher in the occipital cortex of ex-MDMA users. The combined results of this study suggest a compensatory upregulation of post-synaptic 5-HT 2A receptors in the occipital cortex of ex-MDMA users due to low synaptic 5-HT levels.
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