General pharmacological properties of YJA20379-8, a new H+/K+-ATPase inhibitor with anti-ulcer activities

The general pharmacological properties of YJA20379-8 (3-butyryl-4-[(R)-1-me thylbenzylamino]-8-ethoxy-1,7-naphthyridine, CAS 187654-40-6), a new H+/K+- ATPase Inhibitor with anti-ulcer activities, were investigated in mice, rat s and guinea pigs. YJA20379-8 at oral doses of 25, 50 and 100 mg/kg did not affect the locomotor activity, hexobarbital hypnosis and motor coordinatio n in mice. The drug did not have analgesic action and anticonvulsant action at the doses of 100 mg/kg p.o. The respiration and blood pressure were not affected at 10 mg/kg i.v. In rats. YJA20379-8 at 2 X 10(-4) g/ml did neith er produce any contraction nor relaxation of isolated organs, such as guine a pig Ileum, rat fundus, rat uterus and guinea pig vas deferens, and the dr ug antagonized the contractile responses to several spasmogens, such as ace tylcholine, histamine, serotonin, L-phenylephrine, oxytocin and BaCl2. The drug up to 100 mg/kg p.o. did not affect pupil size and the intestinal prop ulsion of mice. And it did not show an anticarrageenan action at 100 mg/kg. In this general pharmacology study, hypothermic effect In mice, retardatio n in gastric emptying in rats, decreases in urine excretion In rats at oral doses of 50 and too mg/kg of YJA20379-8 and the spasmolytic activity could be found. However, no other effects were exhibited at a high oral dose of 100 mg/kg in animals in this study.