Guanethidine類似化合物の薬理学的研究 (第1報)

〔2-(Hexahydro-1-azepinyl)ethyl〕guanidine Sulfateの降圧作用

抄録

Action on blood pressure, pharmacological actions in general, acute toxicity were comparatively examined in guanethidine (I) and the compound formed by changing its eight-membered ring to a seven-membered ring, [2-(hexahydro-1-azepinyl)ethyl]guanidine sulfate (II).
A lasting hypotensive action on rabbits and albino rats was seen in I but it raised blood pressure of cats. II showed lasting depression of blood pressure in rabbits and cats and temporary depression in rats but raised the blood pressure of dogs. Hypotensive action of II in rabbits was not inhibited by hexamethonium or atropine but was inhibited by reserpine. Hypertensive action of adrenaline and noradrenaline in rabbits, cats, and dogs is augmented by II. II showed increased amplitude of excised toad heart in a low concentration but showed no marked action on excised vascular muscle, peripheral blood vessel, skeletal muscle, and excised intestine. LD₅₀ of II in mice was 97.4mg./ kg. by intravenous injection, 887 (776-1088)mg./kg. by subcutaneous injection, and 2000-3000mg./kg. by oral administration, the toxicity being not so strong.