Schweri M M, Jacobson A E, Lessor R A, Rice K C
J Neurochem. 1987 Jan;48(1):102-5. doi: 10.1111/j.1471-4159.1987.tb13132.x.
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 microM 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.
美沙非（1-[1-(3-异硫氰酸苯酯基)环己基]-哌啶）是苯环利定的一种衍生物，在芳香环的间位含有一个异硫氰酸酯基团，在抑制兴奋药物[3H]苏式-(+/-)-甲基苯丙胺与大鼠纹状体组织粗突触体膜结合的能力方面，与其母体化合物（苯环利定）相似（苯环利定和美沙非的IC50分别为1.4和6.2微摩尔）。然而，与苯环利定不同的是，美沙非似乎以不可逆的方式抑制放射性标记兴奋药物的结合，因为在测定[3H]苏式-(+/-)-甲基苯丙胺的结合之前，对经美沙非处理的组织进行反复洗涤时，兴奋药物结合的抑制程度并未降低。这一发现表明，美沙非可能是研究兴奋药物作用分子基础的一种有用工具。
