Stereospecificity of an opiate action on the excitable membrane of frog skeletal muscle fibres

Abstract

Intracellular microelectrode studies were conducted to examine the actions of the optical isomers levorphanol and dextrorphan on the isolated frog sartorius muscle preparation. Both isomers, in bath concentrations which had minimal effect on action potential amplitude and gNa (3 × 10 −5 M), caused a large depression of gK. High bath concentrations (3 × 10 −4 M) of both drugs caused an initial depression of sodium and potassium conductance processes, gNa and gK, respectively, however only levorphanol, but not dextrorphan, could produce a specific, late-occurring depression of gNa that could be blocked by the opiate antagonists, nalorphine or naloxone. These findings indicate that the late-occurring depressant effect on gNa is stereospecific and reinforce previous findings which demonstrated that opiate drugs interact with opiate receptors associated with the sodium channels of the frog muscle fibre membranes.