Quantitative structure-activity studies of substituted benzyl chrysanthemates: 8. Physicochemical properties and neurophysiological effects on membrane potentials of crayfish giant axon

Abstract

The neurophysiological actions of a set of substituted benzyl (1 R)-trans-chrysanthemates and related compounds on the membrane potential of the crayfish giant axon were observed using an intracellular microelectrode. These compounds had one or both of two effects, deceleration of the falling phase of the action potential or elevation of the depolarizing after-potential. The potency of a certain range of compounds to decelerate the rate of the falling phase is mostly determined by the electron-releasing effect of substituents on the aromatic ring. The rate of development of each symptom evaluated in terms of half the time required to reach the maximum response decreased with the hydrophobicity of the compound.