脑循环中内皮素-A受体的特性研究

Characterization of endothelin-A receptors in the cerebral circulation.

作者信息

Adner M, You J, Edvinsson L

机构信息

Department of Experimental Research, Malmö General Hospital, Sweden.

出版信息

Neuroreport. 1993 Apr;4(4):441-3. doi: 10.1097/00001756-199304000-00026.

DOI:10.1097/00001756-199304000-00026

PMID:8499606

Abstract

Endothelin-1 (ET-1), a 21-amino acid peptide produced by the vascular endothelium, mediates contraction. In the present study we demonstrate that both ET-1 (Emax: 238 +/- 29% of potassium contraction) and ET-2 (Emax: 231 +/- 36%) produce strong concentration-dependent contractions of circular segments of guinea-pig middle cerebral artery, whereas ET-3 has only weak effects (Emax: 32 +/- 13%). FR 139317 (10(-6) M), a selective endothelinA (ETA) receptor antagonist, shifted the ET-1 response curve to the right (pD2:7.86 +/- 0.09 with and 8.76 +/- 0.09 without the antagonist) in a competitive manner (pA2 = 6.83). These findings are the first to show the presence of ETA receptors in cerebral vessels.

摘要

内皮素 -1（ET -1）是一种由血管内皮产生的21个氨基酸的肽，可介导血管收缩。在本研究中，我们证明ET -1（最大效应：钾离子收缩的238±29%）和ET -2（最大效应：231±36%）均可使豚鼠大脑中动脉环段产生强烈的浓度依赖性收缩，而ET -3的作用较弱（最大效应：32±13%）。选择性内皮素A（ETA）受体拮抗剂FR 139317（10⁻⁶ M）以竞争性方式使ET -1的反应曲线右移（有拮抗剂时pD2为7.86±0.09，无拮抗剂时为8.76±0.09）（pA2 = 6.83）。这些发现首次表明脑血管中存在ETA受体。