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• W2076262810 abstract "Abstract A series of cyclic 2′,3′-nucleotides, cyclic 3′,5′-nucleotides and derivatives of cyclic 3′,5′-adenosine monophosphate (cyclic AMP) with a substituent at the C-8 position were investigated as inhibitors of partially purified cyclic AMP phosphodiesterases (PDE) of cat heart and rat brain. The assays were carried out at a substrate concentration (0.06 μM) where the contribution to the total enzyme activity by phosphodiesterases with K m values for cyclic AMP above 100 μM was insignificant; consequently the activity measured was that of low K m enzymes. Cyclic 3′,5′-guanosine monophosphate (cyclic GMP) and cyclic 3′,5′-inosine monophosphate (cyclic IMP) were shown to be the most potent inhibitors of PDE of cat heart (I 50 = 1 and 2 μ M, respectively). Of the cyclic AMP derivatives tested that have a substituent at the C-8 position, 8-bromo cyclic AMP was the most potent inhibitor; next most potent were the derivatives with a sulfur atom, whereas derivatives with oxygen- or nitrogen-containing substituents were the least potent inhibitors of PDE of cat heart or rat brain. Most of the cyclic nucleotides that were tested were more potent inhibitors of the PDE of cat heart than that of PDE of rat brain. The kinetic properties of PDE of cat heart were also investigated in the presence of cyclic GMP, cyclic IMP and 8-bromocyclic AMP. All three compounds were found to be competitive inhibitors, with apparent K i values of 0.51, 2.3 and 20 μM respectively. The possible pharmacologic role of cyclic nucleotides is discussed." @default.
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• W2076262810 date "1973-01-01" @default.
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• W2076262810 title "Effect of cyclic nucleotides on activity of cyclic 3′,5′-adenosine monophosphate phosphodiesterase" @default.
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• W2076262810 doi "https://doi.org/10.1016/0006-2952(73)90275-x" @default.
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