Pharmacological Studies on Antispasmodics. I. Selectivity to Antispasmodic Activity of Diarylmethylene-5-methyl-trans-quinolizidinium Bromides

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Abstract
Pharmacological properties of 3-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide (HSR-902), 2-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide (HSR-911), 3-diphenylmethylene-5-methyl-trans-quinolizidinium bromide (HSR-405) and 2-diphenylmethylene-5-methyl-trans-quinolizidinium bromide (HSR-402), new antispasmodic agents, were compared with those of atropine and butylscopolamine bromide. These antispasmodic agents shifted the dose-response curve of acetylcholine chloride (ACh) in parallel to the right without decreasing the maximal response in isolated guinea pig ileum, and the Schild plots were linear. The order of potency to antagonize the spontaneous motility of guinea pig ileum was: HSR-91 .**GRAPHIC**. atropine > HSR-402 > HSR-902 .mchgt. HSR-405 > butylscopolamine bromide. The order of potency to mydriatic activity of rat or mouse was: atropine > HSR-911 .**GRAPHIC**. HSR-402 .mchgt. HSR-405 > HSR-902 > butylscopolamine bromide. The order of potency to inhibit pilocarpine induced salivation of guinea pig or mouse was: atropine .mchgt. HSR-911 > HSR-402 > HSR-902 > HSR-405 > butylscopolamine bromide. Antagonisms of these antispasmodic agents against ACh were competitive, and the selectivity to antispasmodic activity of HSR-902 might be the highest among the antispasmodic agents including atropine and butylscopolamine bromide.