General pharmacological properties of YJA 20379-1, a novel proton pump inhibitor with antiulcer activities

The general pharmacological properties of YJA 20379-1 (2-amino-4,5-dihydro- 8-phenylimid-azo[2,1-b]thiazolo[4,5-g]benzothiazole), a novel proton pump i nhibitor with antiulcer activities, were investigated in mice, rats, guinea pig and rabbits. YJA 20379-1 at oral doses of 50, 100 and 200 mg/kg did no t affect the general behaviour, hexobarbital hypnosis, motor coordination a nd body temperature in mice. The drug does not have analgesic and anticonvu lsant action at 200 mg/kg p.o. The locomotor activity was not affected at 1 00 mg/kg p.o., but at 200 mg/kg, the activity was suppressed. YJA 20379-1 ( at 3 x 10(-4) g/ml) did neither produce any contraction nor relaxation of i solated organs such as rat fundus, rat uterus, guinea pig ileum and guinea Dig vas deferens, and the drug did not antagonize the contractile response to several spasmogens, such as histamine, acetylcholine, serotonin and oxyt ocin, and the drug up to 200 mg/kg p.o. did not affect pupil size of mice. The intestinal propulsion in mice was not affected up to 200 mg/kg p.o. The gastric emptying in rats was not affected at 100 mg/kg p.o., even if retar dation in gastric emptying occurred at 200 mg/kg. YJA 20379-1 did not show anti-inflammatory action nor did it affect urinary excretion up to 200 mg/k g p.o. From these results, it is suggested that YJA 20379-1 at the high dos e of 100 mg/kg p.o. may not exert any adverse effects.