BINDING OF STRYCHNINE AND STRYCHNINE ANALOGS TO SYNAPTIC-MEMBRANES OF RAT BRAIN-STEM AND SPINAL-CORD

Google Scholar
  • 1 January 1977
    • journal article
    • research article
    • Vol. 201  (2) , 326-331
Abstract
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 .mu.M unlabeled strychnine, was saturable with a Kd value of 12 nM. The 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. Neither the biological activities in the mouse nor the binding activity in vitro correlated with the n-octanol-water distribution coefficients. The concept is supported that the 3H-strychnine binding site detected in vitro is the site of pharmacological activity in vivo.