The glycine synaptic receptor: evidence that strychnine binding is associated with the ionic conductance mechanism

Abstract

The ability of a series of anions to inhibit [(3)H]strychnine binding to spinal cord synaptic membranes correlates closely with their neurophysiologic capacity to reverse inhibitory postsynaptic potentials in the mammalian spinal cord. Seven neurophysiologically active anions are also effective inhibitors of [(3)H]strychnine binding with mean effective doses ranging from 160 to 620 mM. Seven other anions that are ineffective neurophysiologically also fail to alter strychnine binding. Chloride inhibits strychnine binding in a noncompetitive fashion. Hill plots of the displacement of [(3)H]strychnine by chloride give coefficients of 2.3-2.7. The inhibition of strychnine binding by these anions suggests that strychnine binding is closely associated with the ionic conductance mechanism for chloride in the glycine receptor.