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Stereoselective pharmacological effects of lysergic acid amides possessing chirality in the amide su

Stereoselective pharmacological effects of lysergic acid amides possessing chirality in the amide su

  1. Gradient
    David E. Nichols, A. Montea, X. Huangb and D. Marona-Lewickab


    Studies of the affinities for serotonin 5-HT2A and 5-HT1A receptor subtypes of lysergic acid amides prepared from chiral 2-aminoalkanes showed a stereoselective preference at both receptor types for the amides with alkyl groups containing the R configuration. The 5-HT2A receptor was less tolerant of long alkyl groups than was the 5-HT1A subtype. In vivo assays in rats trained to discriminate LSD from saline also showed that amides with alkyl groups having the R configuration were most potent.