Brewster A G, Caulkett P W, Jessup R
J Med Chem. 1987 Jan;30(1):67-70. doi: 10.1021/jm00384a012.
(5Z)-7-(2,2-Dimethyl-4-phenyl-1,3-dioxan-cis-5-yl)heptenoic acid (2) was found to be a specific, competitive thromboxane A2 receptor antagonist that acts at platelet, vascular, and pulmonary receptors. No antagonism was detected at receptors for prostacyclin, SRSA, norepinephrine, and serotonin. The synthesis of a series of analogues is described; activity at the thromboxane receptor was observed in cis-substituted compounds but not in their trans counterparts. Compound 2 inhibited the bronchoconstriction induced by a stable thromboxane mimetic in the anesthetized guinea pig.
(5Z)-7-(2,2-二甲基-4-苯基-1,3-二氧杂环己烷-顺-5-基)庚烯酸(2)被发现是一种特异性、竞争性血栓素A2受体拮抗剂，作用于血小板、血管和肺受体。在前列环素、慢反应物质A、去甲肾上腺素和5-羟色胺的受体上未检测到拮抗作用。描述了一系列类似物的合成；在顺式取代的化合物中观察到了对血栓素受体的活性，而在其反式对应物中未观察到。化合物2抑制了麻醉豚鼠中由稳定的血栓素模拟物诱导的支气管收缩。
