[Pharmacological studies on antispasmodics. IV. Ganglion blocking activity of 3-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide (HSR-902) and the correlation between its blocking activity and its inhibitory activity towards urinary bladder contraction (author's transl)].
The ganglion blocking activity of HSR-902, a new antispasmodic agent, was compared with those of atropine sulfate, butylscopolamine bromide, timepidium bromide, prifinium bromide and hexamethonium chloride. These agents inhibited the postganglionic action potential induced by preganglionic cervical sympathetic nerve stimulation in cat and the order of potency was as follows: hexamethonium chloride much greater than timepidium bromide in equilibrium with butylscopolamine bromide greater than prifinium bromide greater than HSR-902 much greater than atropine sulfate. Moreover, the inhibitory activities were correlated with the inhibitory activities of these agents on urinary bladder contraction induced by pelvic nerve stimulation in cat which had been demonstrated in a previous report. On the nictitating membrane contraction induced by postganglionic cervical sympathetic nerve stimulation in cat, HSR-902 alone exhibited a slight inhibition. HSR-902, as well as tolazoline hydrochloride, an alpha-blocking agent, shifted the dose-response curve of noradrenaline-contraction in parallel to the right without decreasing maximal response in the isolated aorta of guinea pig, and the plots of Schild were found to be linear. These results suggested that the weak inhibitory activity of HSR-902 on urinary bladder contraction would be due to the weakness of its ganglion blocking activity and that it is a new antispasmodic agent with a slight alpha-blocking activity.
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D002415:Cats; D005260:Female; D005730:Ganglionic Blockers / Q000494:pharmacology*; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009541:Nictitating Membrane / Q000187:drug effects; D010276:Parasympatholytics / Q000494:pharmacology*; D011807:Quinolizines / Q000494:pharmacology*; D001743:Urinary Bladder / Q000187:drug effects*
D005730:Ganglionic Blockers; D010276:Parasympatholytics; D011807:Quinolizines; C030950:thiaton