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General Pharmacological Properties of the New +/K+ ATPase Inhibitor DBM-819  

Park, Woo-Kyu (Pharmaceutical Screening Research Laboratory, Korea Research Institute of Chemical Technology)
Kong, Jae-Yang (Pharmaceutical Screening Research Laboratory, Korea Research Institute of Chemical Technology)
Kim, Hyun-Jung (Pharmaceutical Screening Research Laboratory, Korea Research Institute of Chemical Technology)
Lee, Dong-Ha (Dongbu Hannonog Chemical Co. Ltd.)
Lim, Hong (Dongbu Hannonog Chemical Co. Ltd.)
Cheon, Hyae-Gyeong (Pharmaceutical Screening Research Laboratory, Korea Research Institute of Chemical Technology)
Publication Information
Biomolecules & Therapeutics / v.10, no.1, 2002 , pp. 19-24 More about this Journal
Abstract
The effects of a newly synthesized $H^+/K^+$ ATPase inhibitor,1-(2-methyl-4-methoxypheny)-4-[(3-hy-droxypropyl)amino] -6-methyl-2,3-dihydropyrrolo (3,2-c) quinoline (DBM-819) , on the central nervous system, isolated smooth muscle, cardiovascular and digestive systems and renal function were investigated in various experimental animals. Oral administration of DBM-819 had no effect on the central nervous system except body temperature of mice slightly decreased at doses of 15 and 50 mg/kg. DBM-819 produced a moderate analgesic effect in acetic acid-induced writhing test in mice at 50 mg/kg (p.o.). In conscious rats, DBM-819 (15 and 50 mg/kg, p.o.) showed a slight increase in blood pressure and a small decrease in heart rate. DBM-819 had an significant effect on agonist-induced contraction of guinea pig ileum at $1.5{\times}10^{-5}g/ml.$ No significant effect of DBM-819 (5 and 15 mg/kg, i.p) on urinary volume or urinary excretion of $Na^+,\;K^+$ and Cl- was observed in rats. DBM-819 had no significant effect on intestinal transport of a semisolid meal in mice at 15 and 50 mg/kg (p.o.). These findings suggest that DBM-819 exerts no significant pharmacological effects on the central nervous system and renal function at 15 mg/kg (p.o.), but produces some effects on the smooth muscle and circulatory system.
Keywords
DBM-819; $H^+/K^+$ ATPase; general pharmacology;
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