鎮痙薬の研究 (第7報) 4-Benziloyloxy- and 4-(Xanthene-9-carbonyloxy)-1-(1,3-dioxolan-2-ylmethyl)-1-methylpiperidinium塩の薬理作用

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An investigation on the structure-activity relationship with respect to spasmolytic activity of 4-acyloxy-1-alkyl-1-(1,3-dioxolan-2-ylmethyl) piperidinium derivatives (1) has led to the development of 4-acyloxy-1-alkyl-1-(1,3-dioxolan-2-ylmethyl) piperidinium derivatives (2) having further potent spasmolytic activity. The compounds (1 and 2) have two geometrical stereoisomers (trans and cis) attributable to the difference of the configuration at C4-position and tetravalent nitrogen atom of piperidine ring. The trans isomers of 1 and 2 exhibited potent activity than the corresponding cis ones. From the trans-isomers (2), 4-benziloyloxy-1-(1,3-dioxolan-2-ylmethyl)-1-methylpiperidinium bromide (2a) and 1-(1,3-dioxolan-2-ylmethyl)-1-methyl-4-(xanthene-9-carbonyloxy) piperidinium bromide (2b) were selected and subjected to examination for pharmacological properties, acute toxicity, antisialagogic activity, mydriatic activity and spasmolytic activity based on the inhibition of the spontaneous movement by using in situ rabbit stomach. The spasmolytic activity of the trans-2a and 2b were considerably potent than that of atropine sulfate and 8-butylscopolaminium bromide (BSB). Safety range of the trans-2b in terms of the spasmolytic activity for acute toxicity, antisialagogic activity and mydriatic activity could be evaluated larger than that of atropine sulfate and BSB.
社団法人日本薬学会の論文
1985-10-25