Ring-substituted amphetamine interactions with neurotransmitter receptor binding sites in human cortex.
The binding affinities of 3 ring-substituted amphetamine compounds were determined at 9 neurotransmitter binding sites in human cortex. (+/-)-3,4-Methylenedioxyamphetamine (MDA), (+/-)-3,4-methylenedioxyethamphetamine (MDE), and (+/-)-3,4-methylenedioxymethamphetamine (MDMA or 'Ecstasy') all display highest affinity (approximately 1 microM) for the recently identified 'DOB binding site' labeled by [77Br]R(-)4-bromo-2,5-dimethoxyphenylisopropylamine [( 77Br]R(-)DOB). MDA displays moderate affinity (4-5 microM) for the 5-hydroxytryptamine1A (5-HT1A), 5-HT1D, and alpha 2-adrenergic sites in human cortex. MDE and MDMA display lower affinity or are inactive at all other sites tested in the present study. These observations are discussed in relation to the novel psychoactive effects of the ring-substituted amphetamines.
Pierce
P A
PA
Department of Neurology, Stanford University Medical Center, CA 94305.
Peroutka
S J
SJ
D015104:3,4-Methylenedioxyamphetamine / Q000031:analogs & derivatives / Q000494:pharmacology*; D000662:Amphetamines / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D018817:N-Methyl-3,4-methylenedioxyamphetamine; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism*
D000662:Amphetamines; D017981:Receptors, Neurotransmitter; D015104:3,4-Methylenedioxyamphetamine; D018817:N-Methyl-3,4-methylenedioxyamphetamine; C051800:3,4-methylenedioxyethamphetamine