Eperisone, an antispastic agent, possesses vasodilating actions on the guinea-pig basilar artery

J Pharmacol Exp Ther. 1985 Dec;235(3):757-63.


The effects of eperisone, an antispasmodic, on the electrical and mechanical properties of smooth muscle cells of the guinea-pig basilar artery were investigated. Eperisone (below 50 microM) did not modify the membrane potential, membrane resistance, excitatory junction potential evoked by perivascular nerve stimulation or the K- and 5-hydroxytryptamine-induced depolarizations. However, in concentrations over 10 microM, this agent reversibly blocked the spontaneously generated and evoked action potentials in the presence of 5 to 8 mM tetraethylammonium. The contractions evoked by high concentrations of K, 5-hydroxytryptamine or direct muscle stimulation in the presence of tetraethylammonium were dose dependently inhibited by eperisone, in concentrations over 1 microM. In Ca-free 2 mM ethylene glycol bis(beta-aminoethyl ether)-N,N'-tetraacetic acid-containing solution, 5-hydroxytryptamine produced only a single contraction. Eperisone inhibited this contraction to the same extent as that observed in the presence of Ca. These results indicate that eperisone possesses the property of a Ca antagonist on smooth muscle tissues of the guinea-pig basilar artery, in addition to the action of antispastic agent, i.e., this agent blocks the voltage-dependent influx of Ca at the smooth muscle membrane, but not at the nerve terminals, and inhibits the action of Ca in cells through inhibition of the contractile protein.

MeSH terms

  • Animals
  • Basilar Artery / drug effects
  • Calcium Channel Blockers / pharmacology
  • Egtazic Acid / pharmacology
  • Electric Stimulation
  • Female
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Membrane Potentials / drug effects
  • Muscle, Smooth, Vascular / drug effects*
  • Muscle, Smooth, Vascular / physiology
  • Parasympatholytics / pharmacology*
  • Potassium / pharmacology
  • Propiophenones / pharmacology*
  • Serotonin / pharmacology
  • Tetraethylammonium Compounds / pharmacology
  • Vasoconstriction / drug effects
  • Vasodilator Agents / pharmacology*


  • Calcium Channel Blockers
  • Parasympatholytics
  • Propiophenones
  • Tetraethylammonium Compounds
  • Vasodilator Agents
  • eperisone
  • Serotonin
  • Egtazic Acid
  • Potassium