[3H]Monoamine releasing and uptake inhibition properties of 3,4-methylenedioxymethamphetaimne and p-chloroamphetamine analogues

摘要: Abstract The ability of several 3,4-methylenedioxymethamphetamine (MDMA) analogues to inhibit the uptake [3H]serotonin (5-HT), dopamine (DA) and norepinephrine (NE) into synaptosomes was examined. In addition, compounds [3H]-HT DA from rats pretreated with reserpine (5 mg/kg i.p., 16 h pretreatment) compared control experiments. All test were found be potent releasers non-vesicular 5-HT (the IC50 significantly smaller than IC50). range inhibitory activity corresponds well small ED50 values substitute in drug discrimination experiments animals trained discriminate MDMA or S-(+)-N-methyl-1-(1,3-benzodioxol-5-yl)-2-aminobutane (S-MBDB) saline. contrast, there a wide potency for inhibition NE uptake. appeared pure inhibitors while others DA. Several very selective over inhibition, including 3-methoxy-4-methylamphetamine (MMA) 5-methoxy-6-methyl-2-aminoindan (MMAI). A correlation noted between neurotoxic potential some their relative induce release catechol metabolites methylenedioxy-substituted also showed monoamine releasing properties, suggesting that metabolism may play role actions these drugs. present data support hypothesis drug-stimulated is primarily responsible discriminative cue MDMA.