Effect of dantrolene sodium on the contractility of rabbit jejunum in vitro.
The effect of dantrolene sodium on the spontaneous contractions of rabbit jejunum was studied in vitro. Dantrolene sodium (4.5 x 10(6) to 4.5 10(4) M) reversibly decreased the amplitude of contractions in a dose-dependent manner. ED50 was found to be about 7.9 x 10(-5) M. Its effect was biphasic in that a period of potentiation preceded that of suppression of contractions. Lowering or increasing (2.5 fold in each direction) the calciumm concentration of bathing media did not affect the suppression of contraction caused by dantrolene sodium to any significant degree. Caffeine but not quinine was found to be able to restore the activity of the intestine to normal after a 50% inhibition caused by dantrolene sodium. Dantrolene sodium, verapamil and nifedipine were able to shift the dose-response curves of calcium in potassium-polarized rabbit jejunum to the right and pA2 values were found to be 4.18, 7.76 and 8.47 respectively. These data indicate that the effect of dantrolene on smooth muscle is mediated via inhibition of calciu movement across the membrane.
D000818:Animals; D002110:Caffeine / Q000494:pharmacology; D002118:Calcium / Q000037:antagonists & inhibitors / Q000494:pharmacology; D003620:Dantrolene / Q000494:pharmacology*; D005260:Female; D066298:In Vitro Techniques; D007583:Jejunum / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects; D009543:Nifedipine / Q000494:pharmacology; D011817:Rabbits
D002110:Caffeine; D003620:Dantrolene; D009543:Nifedipine; D002118:Calcium