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Differential phospholipase C activation by phenylalkylamine serotonin 5-HT2A receptor agonists

Differential phospholipase C activation by phenylalkylamine serotonin 5-HT2A receptor agonists

  1. chrisn
    Journal of neurochemistry 2005, Vol.95(6), pp.1575-84

    Parrish, Jason C ; Braden, Michael R ; Gundy, Emily ; Nichols, David E


    Experiments compared a series of phenethylamine hallucinogens with their phenylisopropylamine analogues for binding affinity and ability to stimulate serotonin 5-HT2A receptor-mediated hydrolysis of phosphatidyl inositol in cells expressing cloned rat and human 5-HT2A receptors.

    Compounds studied included: 2C-B, 2C-I, 2C-T-2, 2C-TFM, 5-HT (serotonin), Aleph-2, DOB, DOI, DOTFM, PEA, PIA, PLC, TFMfly, and TMA.

    The data found supported the hypothesis that phenylisopropylamines have higher hallucinogenic potency than their phenethylamine analogues primarily because they have higher intrinsic activities at 5-HT2A receptors.