Metaphit Irreversibly Inhibits [3H]threo- (±)-Methylphenidate Binding to Rat Striatal Tissue

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Abstract
Metaphit {1-[1-(3-isothiocyanatophenyl)cyclohexyl]-piperidine}, a derivative of phencyclidine that contains an isothiocyanate group on the meta position of the aromatic ring, resembles its parent compound (phencyclidine) in its ability to inhibit the binding of the stimulant drug [3H]threo-(.+-.)-methylphenidate to crude synaptosomal membranes from rat striatal tissue (IC50=1.4 and 6.2 .mu.M for phencyclidine and Metaphit, respectively). Unlike phencyclidine, however, Metaphit appears to inhibit binding of the radiolabeled stimulant in an irreversible manner, as the degree of inhibition of binding of the stimulant does not diminish when the Metaphit-treated tissue is subjected to repeated washings before determination of the binding of [3H]threo-(.+-.)-methylphenidate. This finding suggests that Metaphit may be a useful tool in the study of the molecular basis of stimulant action.