Hogaboom G K, Mong S, Wu H L, Crooke S T
Biochem Biophys Res Commun. 1983 Nov 15;116(3):1136-43. doi: 10.1016/s0006-291x(83)80261-7.
Using [3H]-leukotriene C4 ([3H]-LTC4) and [3H]-leukotriene D4 ([3H]-LTD4), specific peptidoleukotriene receptors have been identified in membranes derived from guinea-pig lung. In the presence of 0.1 mM guanyl-5'-yl-imidodiphosphate, which completely inhibits [3H]-LTD4 binding, [3H]-LTC4 binding was protein- and temperature-dependent, reached equilibrium within 15 minutes at 20 degrees C and was reversible. Guanine nucleotides had no effect on the [3H]-LTC4 binding. Competition studies with [3H]-LTC4, peptidoleukotrienes C4, D4, E4 and the peptidoleukotriene antagonist FPL 55712 revealed an order of potency of leukotriene C4 much greater than E4 greater than D4 greater than FPL 55712. [3H]-LTD4 competition studies indicated an order of potency of LTD4 greater than LTE4 greater than LTC4 much greater than FPL 55712. Bioconversion of [3H]-LTC4, as determined by high performance liquid chromatography, was less than 3 percent. The data suggest the guinea-pig lung may contain biochemically distinct receptors for LTC4 and LTD4.
利用[3H] - 白三烯C4（[3H] - LTC4）和[3H] - 白三烯D4（[3H] - LTD4），在豚鼠肺来源的膜中鉴定出了特异性肽白三烯受体。在完全抑制[3H] - LTD4结合的0.1 mM鸟苷 - 5'-基 - 亚氨基二磷酸存在下，[3H] - LTC4结合具有蛋白质依赖性和温度依赖性，在20℃下15分钟内达到平衡且是可逆的。鸟嘌呤核苷酸对[3H] - LTC4结合没有影响。用[3H] - LTC4、肽白三烯C4、D4、E4和肽白三烯拮抗剂FPL 55712进行的竞争研究表明，白三烯C4的效力顺序远大于E4大于D4大于FPL 55712。[3H] - LTD4竞争研究表明，LTD4的效力顺序大于LTE4大于LTC4远大于FPL 55712。通过高效液相色谱法测定，[3H] - LTC4的生物转化率小于3%。数据表明豚鼠肺可能含有对LTC4和LTD4具有生化差异的受体。
