BQ-123对大鼠输精管中内皮素-1和内皮素-3的不同作用：非典型内皮素受体的证据
Differential effects of BQ-123 against endothelin-1 and endothelin-3 on the rat vas deferens: evidence for an atypical endothelin receptor.
作者信息
Eglezos A, Cucchi P, Patacchini R, Quartara L, Maggi C A, Mizrahi J
机构信息
Pharmacology Department, Laboratori Guidotti S.p.A, Pisa, Italy.
出版信息
Br J Pharmacol. 1993 Jul;109(3):736-8. doi: 10.1111/j.1476-5381.1993.tb13635.x.
Abstract
- Endothelin-1 and endothelin-3 enhanced concentration-dependently the rat vas deferens twitch response to electrical stimulation, endothelin-1 being three times more potent. Sarafotoxin S6c was at least 200 times less active than endothelin-1. 2. The response to endothelin was antagonized in a competitive manner by the supposedly selective ETA receptor antagonist, BQ-123 (pA2:7.0 +/- 0.1). In contrast, the endothelin-1 concentration-response curve was only shifted two fold in the presence of 10 microM BQ-123, while no effect was observed at 1 microM. 3. This evidence suggests the rat vas deferens contains an endothelin receptor not conforming to the ETA/ETB receptor subtype classification so far proposed.
摘要
- 内皮素 -1和内皮素 -3均浓度依赖性地增强大鼠输精管对电刺激的抽搐反应，内皮素 -1的作用强度是内皮素 -3的三倍。毒蜘蛛毒素S6c的活性至少比内皮素 -1低200倍。2. 假定的选择性ETA受体拮抗剂BQ -123以竞争性方式拮抗对内皮素的反应（pA2：7.0±0.1）。相比之下，在存在10μM BQ -123的情况下，内皮素 -1浓度 -反应曲线仅向右移动两倍，而在1μM时未观察到影响。3. 这一证据表明，大鼠输精管含有一种不符合目前所提出的ETA/ETB受体亚型分类的内皮素受体。
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Presence of a phosphoramidon-sensitive endothelin-converting enzyme which converts big-endothelin-1, but not big-endothelin-3, in the rat vas deferens.大鼠输精管中存在一种磷酰胺脒敏感的内皮素转化酶，该酶可转化大内皮素-1，但不能转化大内皮素-3。
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BQ-123, cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu), is a non-competitive antagonist of the actions of endothelin-1 in SK-N-MC human neuroblastoma cells.BQ-123，环（-D-色氨酸-D-天冬氨酸-脯氨酸-D-缬氨酸-亮氨酸），是一种在SK-N-MC人神经母细胞瘤细胞中对内皮素-1作用的非竞争性拮抗剂。
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Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor.对ETA受体具有选择性的高效新型内皮素拮抗剂的生物学特性
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