Diisopropyl 1,3-dithiol-2-ylidene melonate(NKK-105)の薬理学的研究-1-一般薬理作用

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We have investigated the general pharmacological activities of diisopropyl 1, 3-dithiol-2-ylidene malonate (NKK-105), and obtained the following results. 1. NKK-105 has shown a transient inhibitory effect on respiration, and lowering of blood pressure in rabbits by intravenous injection by a dose of over 10 mg/kg. 2. It has shown an inhibitory effect on the isolated hearts of guinea pigs with a dose of over 1×10-5g/ml, and had no effects upon preatroinization. 3. It has also shown a same inhibitory effect on the isolated smooth muscles of guinea pig trachial muscle, rabbit ileum, guinea pig ileum, rat uterus and guinea pig vas def erens with a dose of over 1×10-6-1×10-5 g/ml. Muscle contraction induced by acetylcholine, nicotine, oxytocin, noradrenaline and barium chloride or electrical stimulation has been inhibited with pretreatment of NKK-105. 4. On the intestinal ability to transport charcoal meal in the intestine of mice, it has also shown an inhibitory effect with a dose of over 100 mg/kg. 5. NKK-105 has increased excretion of urine and electrolytes in mice and rats with a dose of 10, 50 mg/kg, p.o., however, it has shown an inhibitory tendency with a dose of over 250 mg/kg, p.o.. Additionally, NKK-105 has never had any effect on serum electrolytes with a dose 500 mg/kg, p.o..