749191-14-8Relevant articles and documents
Synthesis and pharmacological evaluation of ring-methylated derivatives of 3,4- (Methylenedioxy) amphetamine (MDA)
Parker, Matthew A.,Marona-Lewicka, Danuta,Kurrasch, Deborah,Shulgin, Alexander T.,Nichols, David E.
, p. 1001 - 1005 (1998)
The three isomeric ring-methylated derivatives of the well-known hallucinogen and entactogen MDA (la) were synthesized and evaluated for pharmacological activity as monoamine-releasing agents and as serotonin agonists. The 2-methyl derivative 2a and the 5-methyl derivative 2b were found to be more potent and more selective than the parent compound in inhibiting [3H]-serotonin accumulation in rat brain synaptosomal preparations. Their activity in vivo was confirmed in rats trained to discriminate serotonin-releasing agents and hallucinogens from saline. The results indicate that compounds 2a,b are among the most potent 5-HT-releasing compounds known and show promise as lead compounds in the search for antidepressant drugs that release serotonin rather than inhibit its uptake.