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AZD0865 is a member of a drug class that inhibits gastric H(+),K(+)-ATPase by K(+)-competitive binding. The objective of these experiments was to characterize the mechanism of action, selectivity and inhibitory potency of AZD0865 in vitro. In porcine ion-leaky vesicles at pH 7.4, AZD0865 concentration-dependently inhibited K(+)-stimulated H(+),K(+)-ATPase(More)
The gastric H+,K+ ATPase--the gastric acid pump--is the molecular target for the class of antisecretory drugs called the proton-pump inhibitors (PPIs). These compounds--omeprazole, lansoprazole, and pantoprazole--contain, as their core structure, 2-pyridyl methylsulfinyl benzimidazole. The H+,K+ ATPase is a heterodimer composed of a 1034-amino acid(More)
A hydrophobic amine, SCH 28080, 2-methyl-8-(phenylmethoxy)imidazo(1,2a)pyridine-3-acetonitrile, previously shown to inhibit gastric acid secretion in vivo and in vitro, was also shown to inhibit basal and stimulated aminopyrine accumulation in isolated gastric glands when histamine, high K+ concentrations, or dibutyryl cAMP were used as secretagogues.(More)
Glial S-100 protein, soluble protein, and DNA were quantitatively studied in brains of gerbils chronically exposed to ethanol in a nutritionally complete fluid diet. Eight different brain areas were studied. After exposure to ethanol for 3 months followed by a 4-month post-treatment ethanol-free period, increased amounts of S-100 protein per wet weight were(More)
Inhalation exposure of adult Mongolian gerbils to 320 ppm of trichloroethylene (TCE) during 8 weeks causes a decrease of soluble proteins per wet weight in frontal cerebral cortex, cerebellar anterior part of the hemispheres and in the posterior part of vermis, as well as in hippocampus, although the levels of S 100, a glial cytoplasmic protein, showed an(More)
The homologous proteins S-100a and S-100b affect the microtubule system in a distinctly different way in the presence of low molar ratios of Zn2+. Assembly of brain microtubule proteins can be almost completely inhibited and rapid disassembly can be induced by low molar amounts of S-100b in the presence of low molar ratios [2-4] of Zn2+. Higher molar ratios(More)
Mongolian gerbils were exposed for 12 months to trichloroethylene (TCE) 50 or 150 ppm or perchloroethylene (PCE) 120 ppm. Vermis posterior of cerebellum and hippocampus were used for measurement of high-affinity uptake and release of 3H-gamma-aminobutyric acid (GABA) and 14C-glutamate, as well as for determination of total free tissue amino acids and(More)
A number of substituted imidazo[1,2-a]pyridines and related analogues were selected for biochemical characterization in vitro against both the purified gastric proton pump enzyme, H+/K(+)-ATPase, and the intact gastric gland. The inhibitory activity in these two in vitro models was then examined for correlation with the gastric antisecretory potency(More)