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ETB 型受体介导了姥鲨(白斑角鲨)主动脉血管平滑肌中内皮素刺激的收缩。

ETB-type receptors mediate endothelin-stimulated contraction in the aortic vascular smooth muscle of the spiny dogfish shark, Squalus acanthias.

作者信息

Evans D H, Gunderson M, Cegelis C

机构信息

Mt. Desert Island Biological Laboratory, Salsbury Cove, ME 04672, USA.

出版信息

J Comp Physiol B. 1996;165(8):659-64. doi: 10.1007/BF00301134.

Abstract

Using various agonists, and the specific antagonist BQ-123, we have examined the sensitivity to endothelin of the vascular smooth muscle of the ventral aorta of the spiny dogfish shark, Squalus acanthias. Human endothelin-1 produced significant contraction of isolated vascular smooth muscle rings, with an EC50 of 10 nmol.l-1. The presence of an intact endothelium did not alter this response but the magnitude of the contraction was greater in rings with an intact endothelium. The response to 0.2 mumol.l-1 endothelin-1 was equivalent to that of 0.1 mmol.l-1 acetylcholine, and significantly greater than that to 80 mmol.l-1 KCl, suggesting high sensitivity even to the heterologous, mammalian peptide. The Hill plot of the contractile response was a straight line with a slope of 1.12, indicating that a single receptor was mediating the response. Endothelin-1, endothelin-3, and sarafotoxin S6c produced similar concentration-response curves, and the response to endothelin-1 was insensitive to the ETA-specific inhibitor BQ-123. Our data are consistent with the hypothesis that the receptor involved in the contractile response to endothelin of shark aortic vascular smooth muscle is of the ETB-rather than the ETA-type.

摘要

我们使用了多种激动剂以及特异性拮抗剂BQ - 123,研究了棘鲨(Squalus acanthias)腹主动脉血管平滑肌对内皮素的敏感性。人内皮素 - 1可使分离的血管平滑肌环产生显著收缩,其半数有效浓度(EC50)为10 nmol·l-1。完整内皮的存在并未改变这种反应,但完整内皮的环中收缩幅度更大。对0.2 μmol·l-1内皮素 - 1的反应等同于对0.1 mmol·l-1乙酰胆碱的反应,且显著大于对80 mmol·l-1氯化钾的反应,这表明即使对异源的哺乳动物肽也具有高敏感性。收缩反应的希尔图是一条斜率为1.12的直线,表明单一受体介导了该反应。内皮素 - 1、内皮素 - 3和芋螺毒素S6c产生了相似的浓度 - 反应曲线,并且对内皮素 - 1的反应对ETA特异性抑制剂BQ - 123不敏感。我们的数据与以下假设一致,即参与鲨鱼主动脉血管平滑肌对内皮素收缩反应的受体是ETB型而非ETA型。

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