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Dopamine D2High receptors stimulated by phencyclidines, lysergic acid diethylamide, salvinorin A, an

Dopamine D2High receptors stimulated by phencyclidines, lysergic acid diethylamide, salvinorin A, an

  1. Anonymous
    Seeman P, Guan HC, Hirbec H.
    Synapse. 2009 Aug;63(8):698-704.

    Although it is commonly stated that phencyclidine is an antagonist at
    ionotropic glutamate receptors, there has been little measure of its potency on other
    receptors in brain tissue. Although we previously reported that phencyclidine stimulated
    cloned-dopamine D2Long and D2Short receptors, others reported that phencyclidine
    did not stimulate D2 receptors in homogenates of rat brain striatum. This study,
    therefore, examined whether phencyclidine and other hallucinogens and psychostimulants
    could stimulate the incorporation of [35S]GTP-g-S into D2 receptors in homogenates
    of rat brain striatum, using the same conditions as previously used to study the
    cloned D2 receptors. Using 10 lM dopamine to define 100% stimulation, phencyclidine
    elicited a maximum incorporation of 46% in rat striata, with a half-maximum concentration
    of 70 nM for phencyclidine, when compared with 80 nM for dopamine, 89 nM
    for salvinorin A (48 nM for D2Long), 105 nM for lysergic acid diethylamide (LSD), 120
    nM for R-modafinil, 710 nM for dizocilpine, 1030 nM for ketamine, and >10,000 nM
    for S-modafinil. These compounds also inhibited the binding of the D2-selective ligand
    [3H]domperidone. The incorporation was inhibited by the presence of 200 lM guanylylimidodiphosphate
    and also by D2 blockade, using 10 lM S-sulpiride, but not by D1
    blockade with 10 lM SCH23390. Hypertonic buffer containing 150 mM NaCl inhibited
    the stimulation by phencyclidine, which may explain negative results by others. It is
    concluded that phencyclidine and other psychostimulants and hallucinogens can stimulate
    dopamine D2 receptors at concentrations related to their behavioral actions.