心脈管系薬に関する研究(第12報)1-tert-Butylamino-3-[o-(tetrahydrofurfuryloxy)-phenoxy]-2-propanol Hydrochloride(Y-6124)の薬理学的性質

概要

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Y-6124,a new adrenergic β-receptor blocking agent, antagonized lipolysis in the isolated fat cells of rats, increase of free fatty acid in rat plasma, and hyperglycemia in mice and rats induced by epinephrine. The compound also possessed an antagonistic activity against response induced by isoproterenol in the duodenum of rats. Y-6124 had a local anesthetic activity, i.e., activities of infiltration, surface and conduction anesthesia. Local anesthetic activity of this compound may contribute to its antiarrhythmic activity. This compound showed a slight diuretic activity, but had no analgenic, anti-inflammatory, or sensitisation activities. Y-6124 did not show any influence on the central and autonomic nervous systems, coagulation and fibrinolysis of the blood, antibody formation, nor estrus cycle in rats, in a dose to expect β-blocking activity of the compound. These results may suggest the possibility of a clinical application of Y-6124 as an adrenergic β-receptor blocking agent.
公益社団法人日本薬学会の論文
1972-08-25