Moncada S, Bunting S, Mullane K, Thorogood P, Vane J R, Raz A, Needleman P
Prostaglandins. 1977 Apr;13(4):611-8. doi: 10.1016/0090-6980(77)90232-5.
Imidazole inhibits the enzymic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes (IC50: 22 MICRONG/ML; DETERMINED BY BIOASSAY). The inhibitor is selective, for prostaglandin cyclo-oxygenase is only affected at high doses. Radiochemical data confirms that imidazole blocks the formation of 14C-thromboxane B2 from 14C-PGH2. Several imidazole analogues and other substances were tested but only 1-methyl-imidazole was more potent than imidazole itself. The use of imidazole to inhibit thromboxane formation could help to elucidate the role of thromboxanes in physiology or pathophysiology.
咪唑可抑制血小板微粒体将内过氧化物（PGG2和PGH2）酶促转化为血栓素A2（IC50：22微克/毫升；通过生物测定法测定）。该抑制剂具有选择性，因为前列腺素环氧化酶仅在高剂量时受到影响。放射化学数据证实，咪唑可阻断14C-PGH2形成14C-血栓素B2。对几种咪唑类似物和其他物质进行了测试，但只有1-甲基咪唑比咪唑本身更有效。使用咪唑抑制血栓素形成有助于阐明血栓素在生理或病理生理中的作用。
