Holme G, Brunet G, Piechuta H, Masson P, Girard Y, Rokach J
Prostaglandins. 1980 Oct;20(4):717-28. doi: 10.1016/0090-6980(80)90110-0.
The effects of synthetic leukotriene C-1 (LTC-1) on isolated guinea pig trachea and ileum have been determined and compared to histamine. LTC-1 produced a slow contraction of the trachea and the ileum with pD2 values of 8.7 +/- 0.1 (n = 14) and 8.5 +/- 0.1 (n = 13), respectively. In comparison, the pD2 values for histamine were 5.6 +/- 0.1 (n = 6) and 6.2 +/- 0.1 (n = 6), indicating LTC-1 was 2-3 orders of magnitude more potent. LTC-1 was antagonised by FPL 55712 with pA2 values of 6.9 +/- 0.1 (n = 5) and 6.4 +/- 0.1 (n = 7) on the trachea and ileum, respectively. Incubation with lipoxidase produced a time and enzyme dependent loss of biological activity and a concurrent shift in U.V. absorption spectrum.
已测定合成白三烯C-1(LTC-1)对豚鼠离体气管和回肠的作用,并与组胺进行比较。LTC-1使气管和回肠缓慢收缩,其pD2值分别为8.7±0.1(n = 14)和8.5±0.1(n = 13)。相比之下,组胺的pD2值为5.6±0.1(n = 6)和6.2±0.1(n = 6),表明LTC-1的效力强2至3个数量级。FPL 55712可拮抗LTC-1,其对气管和回肠的pA2值分别为6.9±0.1(n = 5)和6.4±0.1(n = 7)。与脂氧化酶一起孵育会导致生物活性随时间和酶量而丧失,并同时伴有紫外吸收光谱的变化。