The Effect of Phentolamine and Other Drugs on Rat Brain Phosphodiesterase

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Abstract
A number of derivatives of imidazole, and the imidazoline derivatives phentolamine and tolazoline, were tested for their effect on cyclic AMP phosphodiesterase obtained from rat brain. Phentolamine and tolazoline inhibited the enzyme with phentolamine being the most potent. Histamine and a derivative of triazole (3-β-aminoethyl-1,2,4-triazole) increased enzyme activity about 10%. It is suggested that enzyme inhibition by phentolamine in addition to an α-adrenergic blockade may explain the reported enhancement of certain catecholamine responses. The stimulation of the enzyme by histamine also may exlpain some of the pharmacological actions of histamine.

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