HYPOTENSIVE ACTION OF OPC-1427, A NEW BETA-ADRENERGIC BLOCKING-AGENT IN RATS

Abstract

8-Acetonyloxy-5-[3-{2-(3,4-dimethoxyphenyl)-ethylamino}-2-hydroxypropoxy]-3,4-dihydrocarbostyril (OPC-1427), is a newly synthesized cardioselective .beta.-adrenoceptor blocking agent. The effects of OPC-1427 given i.p. to conscious Kyoto Wistar normotensive (WKR), spontaneous hypertensive (SHR) and DOCA [deoxycorticosterone acetate]-NaCl hypertensive (DOCA rat) rats was studied. Results were compared to findings with propranolol and practolol. OPC-1427 produced a significant hypotensive action in SHR and DOCA rats and this effect was less in WKR. With propranolol and practolol effective hypotensive effects were seen in WKR and DOCA rats but not in the SHR. The efficacy of the hypotensive action of these agents was propranolol > OPC-1427 = practolol in WKR, OPC-1427 > practolol in SHR, and OPC-1427 > practolol = propranolol in DOCA rats. OPC-1427 appears to be a promising .beta.-adrenoceptor blocking agent which exerts a hypotensive state, as demonstrated in hypertensive rats.