Effects of papaverine on human isolated bladder muscle.
Papaverine is a non-specific smooth muscle relaxant and is thought to act at a site beyond the receptor sites on the cell membrane. In this study the relaxing properties of papaverine were tested in isolated muscle strips from the human bladder dome. In carbachol-induced contractions papaverine, even in high concentrations of 10(-4) mol/l had virtually no effects on peak tension generation, whereas the fading was accelerated and the steady state tension at 30 min. was reduced by about 54%. In contrast, high potassium-induced contractions were relaxed by papaverine in a concentration-dependent way; a concentration of papaverine of 10(-4) mol/l produced full relaxation. These findings might possibly be explained if it is assumed that papaverine blocks calcium ion channels in the cell membrane. However, the observation that rather high concentrations of papaverine were necessary to fully relax high potassium contractions and the fact, that papaverine affects cellular cAMP levels separate this drug from more selective calcium channel blockers. The calcium movements responsible for the peak tension generation in carbachol-induced contractions are obviously not affected by papaverine. Although papaverine had little effect on carbachol-induced contractions in vitro it cannot be excluded that the drug is effective in diseases were non-cholinergic mechanisms are involved.
Department of Urology, University of Bochum, FRG.
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Hertle
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Nawrath
D002121:Calcium Channel Blockers; D002217:Carbachol / Q000494:pharmacology; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008875:Middle Aged; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D010208:Papaverine / Q000494:pharmacology*; D011188:Potassium / Q000494:pharmacology; D001743:Urinary Bladder / Q000187:drug effects*
D002121:Calcium Channel Blockers; D002217:Carbachol; D010208:Papaverine; D011188:Potassium