Su T P, Wu X Z
Neurochemistry Unit, National Institute on Drug Abuse, Baltimore, MD 21224.
Neurosci Lett. 1990 Jan 22;108(3):341-5. doi: 10.1016/0304-3940(90)90664-u.
Homogenates from guinea pig vas deferens were examined for possible existence of sigma receptor and phencyclidine (PCP) receptor using a radioligand binding assay. 3H-SKF-10047 bound saturably in the homogenates to a single population of binding sites with a Kd of 311 and a Bmax of 1090 fmol/mg protein. IC50S of several representative sigma in displacing 3H-SKF-10047 from this binding site were very much similar to the IC50S of those drugs in the brain sigma receptor binding assay. A correlation coefficient of 0.96 was obtained when IC50S from vas deferens were compared with those from the brain assay. Attempts to demonstrate PCP receptors in this tissue using [3H]TCP (N-[1-(2-thienyl)cyclohexyl]piperidine), however, yielded negative results. The results indicate that while guinea pig vas deferens contains sigma receptors, PCP receptors may be absent in this tissue.
利用放射性配体结合分析法，检测豚鼠输精管匀浆中是否可能存在σ受体和苯环己哌啶（PCP）受体。3H-SKF-10047在匀浆中与单一结合位点群体呈饱和结合，解离常数（Kd）为311，最大结合容量（Bmax）为1090 fmol/mg蛋白。几种代表性σ配体从该结合位点置换3H-SKF-10047的半数抑制浓度（IC50），与这些药物在脑σ受体结合分析中的IC50非常相似。当比较输精管中的IC50与脑分析中的IC50时，相关系数为0.96。然而，使用[3H]TCP（N-[1-(2-噻吩基)环己基]哌啶）在该组织中检测PCP受体的尝试，结果为阴性。结果表明，豚鼠输精管含有σ受体，但该组织中可能不存在PCP受体。
