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Synthesis and Pharmacological Examination of 1-(3-methoxy-4-methylphenyl)-2-aminopropane and 5-metho

Synthesis and Pharmacological Examination of 1-(3-methoxy-4-methylphenyl)-2-aminopropane and 5-metho

  1. NeuroChi
    The racemate and the enantiomers of 1-(3-methoxy-4-methylphenyl)-2-aminopropan(e6 ) and racemic bmethoxy-&
    methyl-2-aminoindan (11) were teated for stimulus generalization in the two-lever drug-discrimination paradigm.
    Both 6 and 11 were found to Substitute with high potency in 3,4-(methylenedioxy)methamphetamine (1) and
    (S)-1-(1,3-benzodioxo1-5-y1)-2-(methylamino)but(a2n)et rained rats. In the latter assay, both enantiomers of 6 had
    identical potencies, but their dose-response curves were not parallel. Racemic 6, but not 11, partially substituted
    for LSD. Racemic 6 and 11 did not substitute in (8)-amphetamine-trained rata. All of the test compounds were
    potent inhibitors of [SH]-5-HT uptake into synaptosomes in vitro, with the S enantiomer of 6 being most active.
    Rat brain monoamine levels were unaltered 1 week following a single high dose (10 or 20 mg/kg, sc) of 6 or 11, or
    two weeks following a subacute d h g regimen (20 mg/kg, BC, twice a day for 4 days). In addition, radioligand-binding
    parameters in rat brain homogenate with the 5HT uptake inhibitor [aH]paroxetine were unchanged after subacute
    dosing with either racemic 6 or 11. The resulta indicate that compounds 6 and 1 1 have animal behavioral pharmacology
    similar to the methylenedioxy compounds 1 and 2, but that they do not induce the serotonin neurotoxicity that
    haa been observed for the latter two drugs.