Mackerer C R, Kochman R L, Shen T F, Hershenson F M
J Pharmacol Exp Ther. 1977 May;201(2):326-31.
Crude synaptic membranes were isolated from rat pons, medulla and spinal cord by differential centrifugation. The specific binding of [3H]strychnine, obtained by subtracting from the bound radioactivity the amount not displaced by 50 micronm unlabeled strychnine, was saturable with a KD value of 12 nM. The dissociation constants (KD values) for the binding of several strychnine analogs to the strychnine site in vitro were determined and found to be highly correlated with the convulsant and lethal effects in the mouse. However, neither the biological activities in the mouse nor the binding activity in vitro correlated with the n-octanol-water distribution coefficients. The results are in accord with the concept that the [3H]strychnine binding site detected in vitro is the site of pharmacological activity in vivo.
通过差速离心从大鼠脑桥、延髓和脊髓中分离出粗制突触膜。[3H]士的宁的特异性结合通过从结合的放射性中减去50微米未标记士的宁未取代的量获得，其具有12 nM的KD值且可饱和。测定了几种士的宁类似物在体外与士的宁位点结合的解离常数（KD值），发现其与小鼠的惊厥和致死作用高度相关。然而，小鼠体内的生物学活性和体外的结合活性均与正辛醇-水分配系数无关。这些结果与体外检测到的[3H]士的宁结合位点是体内药理活性位点的概念一致。
