ピペラジン誘導体の研究(第4報) : Piperazinoalkyltheophylline誘導体の冠および肢血流に対する作用

概要

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Examinations were made on the effect of 45 kinds of piperazinoalkyltheophylline derivatives (Table I) on the coronary blood flow and peripheral (femoral vein) blood flow, using anesthetized dogs. Acute toxicity (LD_<50>) of these pharmaceutics was examined by intravenous injection into tail vein of mice. The values obtained were calculated into potency index and toxicity index, taking the value of aminophylline, used as the control, as 1. Compounds possessing aralkyl group as the substituent in 4-position of the piperazine ring showed strong increasing action on blood flow of both circulatory systems, the degree of such action differing with the structure of the substituents. Changes in the structure of the bonding bridge between the piperazine ring and theophylline also affected the degree of activity, acylation of the β-hydroxypropylene group resulting in increased activity. Examination of the ratio of potency index on coronary blood flow to that on femoral blood flow suggested that acylation of the hydroxyl group on the bonding bridge increased the peripheral blood flow rather than coronary blood flow. Acute toxicity was generally lower in compounds having a β-hydroxypropylene group as the bonding bridge.
公益社団法人日本薬学会の論文
1969-06-25