Studies on 3,7-Dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191). I. Cyclic 3', 5'-Nucleotide Phosphodiesterase (PDE) and the Inhibitory Effect of BL 191 on PDE in Rat Brain and Heart

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Some properties of cyclic 3', 5'-nucleotide phosphodiesterase (PDE) in the rat cerebral cortex and heart muscle and inhibitory effect of 3,7-dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191) on PDE have been investigated by comparison with theophylline and caffeine as PDE inhibitor. 1) Cyclic adenosine monophosphate (AMP) hydrolysis in the supernate of the cerebral cortex and heart muscle is linear with respect to time (up to 30 min) and protein concentration (up to 150 μg and 400 μg in the incubation medium on the brain and heart respectively). 2) PDE activity obtained in the absence of Mg^<2+> could be increased up to 70 per cent by adding Mg^<2+> with the supernate of the cerebral cortex as the enzyme. 3) Substantial activity was present in all of the fraction although most was contained in the supernate. 4) From typical Lineweaver-Burk plots, K_m values for the supernate of the cerebral cortex and heart muscle were found to be 130 μM and 74 μM respectively. 5) Inhibitory effect of BL 191 on PDE from the rat cerebral cortex supernate was similar to the action of theophylline and was slightly more potent than that of caffeine. The inhibition of BL 191,theophylline and caffeine was noncompetitive ; the K_i was calculated to be 3.0 mM, 3.1 mM and 5.1 mM respectively. The K_i values of 1.65 mM, 1.80 mM and 1.55 mM were found in the heart muscle supernate treated with BL 191,theophylline and caffeine respectively : the type of inhibition was competitive.
公益社団法人日本薬学会の論文
1974-03-25

Studies on 3,7-Dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191). I. Cyclic 3', 5'-Nucleotide Phosphodiesterase (PDE) and the Inhibitory Effect of BL 191 on PDE in Rat Brain and Heart

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