Effect of 3-[2-[4-(o-Methoxyphenyl)-1-piperazinyl]ethyl]-2,4(1H, 3H)-quinazolinedione Monohydrochloride (SGB-1534), an Anthihypertensive Agent, on ^3H-Prazosin and ^3H-p-Aminoclonidine Binding to α_1-and α_2-Adrenoceptors in Dog Brain and Arta

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In order to assess the antihypertensive activities of SGB-1534,3-[2-[4-(o-methoxyphenyl)-1-piperazinyl]ethyl]-2,4-(1H, 3H)-quinazolinedione monohydrochloride, the effect of this drug on the ^3H-prazosin, ^3H-p-aminoclonidine and ^3H-dihydroalprenolol (^3H-DHA) bindings to α_1-, α_2-and β-adrenoceptors in dog brain and aorta was determined by means of radioligand binding assay and compared with that of prazosin. Potent inhibition of ^3H-prazosin binding to α_1-adrenoceptor sites in the brain and the aorta by SGB-1534 was observed (the potency in the brain was almost the same as that prazosin), but the inhibition of ^3H-p-aminoclonidine and ^3H-DHA bindings to α_2-and β-adrenergic binding sites by both SGB-1534 and prazosin was very weak. In addition, a high pA_2 value of α_1-blocking action by SGB-1534 was fornd in a pharmacological experiment. Thus, these results suggest that the inhibitory effect of SGB-1534 at α_1-adrenoceptor binding sites, but not at α_2-or β-adrenozeptor sites, may contribute to the hyprotensive effect.
社団法人日本薬学会の論文
1988-03-25