Abstract
Selective inhibitors of thromboxane (TX) formation have potential utility in the treatment of hypertension, atherosclerosis, thrombosis, myocardial ischemia, cancer metastasis, etc. This class of compounds not only removes TX, a potent vasoconstrictor and inducer of platelet aggregation, but may also enhance the production of a potent vasodilator and inhibitor of platelet aggregation, viz. , prostacyclin (epoprostenol, PGI 2). The specific thromboxane synthetase (TXS) inhibitor 1-benzylimidazole (1-BI) demonstrated a weak and OKY-1581 (OKY) a potent inhibition of TX formation in SHR-derived platelets in vitro . The acute antihypertensive effects produced by 1-BI were marked while those of OKY were less significant in SHR. 1-BI and OKY did not demonstrate an inhibition of PGI 2). formation in SHR-derived aortic rings in vitro . Indomethacin (I), which inhibits the formation of both TX and PGI 2). was not antihypertensive and did not antagonize the blood pressure lowering effects of 1-BI in the present studies. Oral and intravenous dosing with 1-BI, unlike OKY, produced epinephrine reversal in SHR, indicating the blockade of alpha-adrenoceptors. In conclusion, the acute antihypertensiv6 effects of 1-BI in SHR result mainly from alpha-adrenoceptor blockade, not inhibition of TXS activity.
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