Brittain R T, Boutal L, Carter M C, Coleman R A, Collington E W, Geisow H P, Hallett P, Hornby E J, Humphrey P P, Jack D
Circulation. 1985 Dec;72(6):1208-18. doi: 10.1161/01.cir.72.6.1208.
Despite numerous suggestions in the literature that thromboxane A2 is involved in a variety of occlusive vascular diseases, no definitive evidence is available. Arguments have been presented to support the view that such evidence can only come from clinical studies with a highly specific thromboxane receptor-blocking drug. We have now identified such a drug, AH23848, in our laboratories. Preliminary experiments with AH23848, ([1 alpha (Z), 2 beta,5 alpha]-(+/-)-7-[5-[[(1,1'-biphenyl)-4-yl]methoxy]-2-(4-morpholin yl)-3-oxocyclopentyl]-4-heptenoic acid), show that it is a potent, specific thromboxane receptor-blocking drug that is orally active and has a long duration of action. It should be a valuable tool in elucidating any physiologic or pathologic role of thromboxane A2.
尽管文献中有众多观点认为血栓素A2与多种闭塞性血管疾病有关,但尚无确凿证据。有人提出论据支持这样一种观点,即此类证据只能来自使用高度特异性血栓素受体阻断药物的临床研究。我们现已在实验室中鉴定出这样一种药物,AH23848,([1α(Z),2β,5α]-(±)-7-[5-[[(1,1'-联苯)-4-基]甲氧基]-2-(4-吗啉基)-3-氧代环戊基]-4-庚烯酸),初步实验表明它是一种强效、特异性的血栓素受体阻断药物,具有口服活性且作用持续时间长。它在阐明血栓素A2的任何生理或病理作用方面应是一种有价值的工具。