Mayhan W G, Rubinstein I
Department of Physiology and Biophysics, University of Nebraska Medical Center, Omaha 68198-4575, USA.
Int J Microcirc Clin Exp. 1995 Jan-Feb;15(1):48-52. doi: 10.1159/000178949.
Our goal was to examine the effects of endothelin-1 and endothelin-3 on hamster cheek pouch arterioles in vivo in the absence and presence of endothelin receptor antagonists. Endothelin-1 (0.1, 1.0 and 10 pM) and endothelin-3 (0.1 and 1.0 nM) produced dose-related constriction of cheek pouch arterioles which was inhibited by the endothelin ETAB receptor antagonist PD 142893 (Ac-D-Dip-Leu-Asp-Ile-Ile-Trp) and endothelin ETA receptor antagonist PD 147953 [FR 139317: (hexahydro-1H-azepinyl)carbonyl-Leu-(N-Me)-D-Trp- D-2-Pya]. The thromboxane analogue, U-46619 (0.1 and 1.0 nM) also produced dose-related constriction of cheek pouch arterioles, but in contrast to endothelin-1 and endothelin-3 this vasoconstriction was not abolished by endothelin receptor antagonists. These findings suggest that endothelin-1 and endothelin-3 produce marked constriction of cheek pouch arterioles which appears to be mediated by activation of endothelin ETA receptors.
我们的目标是在存在和不存在内皮素受体拮抗剂的情况下，研究内皮素 -1 和内皮素 -3 对仓鼠颊囊小动脉的体内作用。内皮素 -1（0.1、1.0 和 10 pM）和内皮素 -3（0.1 和 1.0 nM）可引起颊囊小动脉剂量相关的收缩，该收缩可被内皮素 ETAB 受体拮抗剂 PD 142893（Ac - D - Dip - Leu - Asp - Ile - Ile - Trp）和内皮素 ETA 受体拮抗剂 PD 147953 [FR 139317：（六氢 -1H - 氮杂环庚烷基）羰基 - Leu -（N - Me）- D - Trp - D - 2 - Pya]抑制。血栓素类似物 U - 46619（0.1 和 1.0 nM）也可引起颊囊小动脉剂量相关的收缩，但与内皮素 -1 和内皮素 -3 不同的是，这种血管收缩不会被内皮素受体拮抗剂消除。这些发现表明，内皮素 -1 和内皮素 -3 可引起颊囊小动脉明显收缩，这似乎是由内皮素 ETA 受体激活介导的。
