Sun F Y, Zhu H, Zhang L M, Xu X R, Zhang A Z
Dept. of Neurobiology, Shanghai Medical University, China.
NIDA Res Monogr. 1986;75:169-72.
Radio-binding assay, bioassay and HPLC detection were used to observe the antagonistic effects of dextrorphan on PCP's actions. Dextrorphan displayed high affinity to PCP receptors and it had weak PCP-like bioactivity, but could antagonize PCP's action dose-dependently in vitro and shift the dose-response curve to the right. PCP increased the contents of norepinephrine in bath medium, which was reversed by dextrorphan. Thus, the results suggest that dextrorphan is a partial antagonist for PCP receptors.
采用放射配体结合试验、生物测定法和高效液相色谱检测法观察右啡烷对苯环己哌啶作用的拮抗效应。右啡烷对苯环己哌啶受体表现出高亲和力，具有较弱的苯环己哌啶样生物活性，但在体外能剂量依赖性地拮抗苯环己哌啶的作用，并使剂量反应曲线右移。苯环己哌啶增加了浴槽培养基中去甲肾上腺素的含量，这一作用可被右啡烷逆转。因此，结果表明右啡烷是苯环己哌啶受体的部分拮抗剂。
