Pharmacological effects of propiverine and its active metabolite, M-1, on isolated human urinary bladder smooth muscle, and on bladder contraction in rats

International Journal of Urology : Official Journal of the Japanese Urological Association
Yutaka SugiyamaShoichi Ueda

Abstract

To investigate the effects of M-1, a major active metabolite of propiverine on the bladder. We have evaluated the effects of M-1 on the contractions induced by carbachol, KCl, CaCl(2), and electrical field stimulation (EFS) in human detrusor smooth muscles, and pelvic nerve stimulation-induced bladder contractions in rats. The effects of M-1 were also compared with the effects of propiverine and tolterodine. Pretreatment with propiverine and tolterodine caused parallel shifts to the right of the concentration-response curves to carbachol. M-1 caused concentration-dependent reduction in the maximum contractile responses induced by carbachol. Although tolterodine did not inhibit the KCl- and CaCl(2)-induced contractions, M-1 and propiverine significantly inhibited these contractions. In the presence of atropine, M-1 and propiverine significantly inhibited the atropine resistant part of the contraction induced by EFS. On the other hand, tolterodine did not have significant inhibitory effects on atropine resistant contractions. Pelvic nerve stimulation induced bimodal phasic and tonic contractions in the rat bladder. M-1 mainly inhibited the phasic contraction. Tolterodine caused a significant inhibition in the tonic contraction, a...Continue Reading

References

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Citations

Feb 26, 2010·Naunyn-Schmiedeberg's Archives of Pharmacology·Stefan ProppingMelinda Wuest
Nov 26, 2009·International Journal of Clinical Practice·L CardozoM Yoshida
Aug 9, 2012·Expert Opinion on Drug Metabolism & Toxicology·Umberto Leone Roberti MaggioreSimone Ferrero

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