Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
THE EFFECTS OF TRAXANOX SODIUM ON CYCLIC AMP PHOSPHODIESTERASE AND THE CONCENTRATION OF CYCLIC AMP IN THE PLASMA OF RATS
Kiyoteru IkegamiShigeru HiranoGen Hasegawa
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1983 Volume 31 Issue 2 Pages 752-755

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Abstract
Traxanox sodium salt pentahydrate (9-chloro-5-oxo-7-(1H-tetrazol-5-yl)-5H-[1] benzopyrano [2, 3-b] pyridine sodium salt pentahydrate, Code No. Y-12, 141) (traxanox sodium) inhibited cyclic AMP phosphodiesterase in the lungs and hearts of rats. The inhibitory effect of traxanox sodium was more potent than that of both theophylline and sodium cromoglycate, but was less potent than that of papaverine. In the low Km (2 μM) enzyme of lungs the inhibition by traxanox sodium was competitive and its inhibition constant (Ki) was 66.7 μM. Intraperitoneal injection of traxanox sodium (100 mg/kg) synergistically enhanced the isoproterenol-induced increase of cyclic AMP in the plasma of rats.
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© The Pharmaceutical Society of Japan
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