TY - JOUR T1 - The binding of strychnine and strychnine analogs to synaptic membranes of rat brainstem and spinal cord. JF - Journal of Pharmacology and Experimental Therapeutics JO - J Pharmacol Exp Ther SP - 326 LP - 331 VL - 201 IS - 2 AU - C R Mackerer AU - R L Kochman AU - T F Shen AU - F M Hershenson Y1 - 1977/05/01 UR - http://jpet.aspetjournals.org/content/201/2/326.abstract N2 - 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. ER -