Adrenergic and Serotonergic Receptor-Blocking Potencies of Terazosin, a New Antihypertensive Agent, as Assessed by Radioligand Binding Assay(Pharmacological)

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To assess the antihypertensive effect of terazosin, 2-[4-(tetrahydro-2-furanyl) carbonyl-l-piperazinyl]-6, 7-dimethoxy-4-quinazolinamine hydrochloride dihydrate, the inhibitory potency of terazosin on ^3H-prazosin, ^3H-p-aminoelonidine, ^3H-dihydroalprenolol (^3H-DHA), ^3H-serotonin and ^3H-ketanserin bindings to α_1-, α_2- and β-adrenergic receptors and 5HT_1,-and-5HT_2 (serotonergic) receptors was examined by using the radioligand binding melhod. The results were compared with those for prazosin and hunazosin. Dog brain and aorta were used in the present study. A high inhibition of ^3H-prazosin binding to α_1-adrenoceptors in dog aorta by terazosin was observed, but the inhibitions of ^3H-DHA, ^3H-p-aminoclonidine. ^3H-serotonin and ^3H-ketanserin bindings by this drug were very weak. l-Terazosin showed the greatest inhibitory effect on ^3H-prazosin binding to α_1-adrenoceptors in dog aorta and brain. These results suggest that an inhibitory effect of terazosin at α_1-adrenoceptor binding sites may contribute to the hypotensive effect ; the α_2- and β-adrenoceptors and the serotonergic binding sites do not appear to be involved.
社団法人日本薬学会の論文
1987-04-25