Plasticity of contractile endothelin-B receptors in human arteries after organ culture

British Journal of Pharmacology
M AdnerL Edvinsson

Abstract

1. The pharmacology and mRNA expression of endothelin (ET) receptors in human omental arteries were characterized by use of functional contractile assays and the reverse transcriptase-polymerase chain reaction (RT-PCR). 2. In freshly obtained segments of human omental arteries, ET-1 and ET-3 induced concentration-dependent contractions which were normalized to the response produced by 60 mM K+. ET-1 produced a maximum contraction (Emax) amounting to 151 +/- 17% of the K+ response. The pEC50 for this agonist was 8.64 +/- 0.17. The effect of ET-3 was less pronounced (Emax: 71 +/- 22% and pEC50: 6.69 +/- 0.17) than that of ET-1. The ET receptors involved were characterized with FR139317 (a selective ETA receptor antagonist), PD 145065 (a mixed ETA and ETB receptor antagonist) and BQ 788 (an ETB receptor antagonist). A high concentration of these antagonists (10 microM) abolished the contractile responses to ET-3, and produced a parallel rightward shift of the ET-1 concentration-response curve without changing the maximal effect. FR139317 and PD 145065 were equally effective while BQ 788 was much less effective. This is consistent with ETA receptors mediating contraction in human omental arteries. 3. Arterial segments cultured for ...Continue Reading

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Citations

Jul 26, 2011·Medical & Biological Engineering & Computing·Samantha M Steelman, Jay D Humphrey
Jan 20, 2004·European Journal of Pharmacology·Angelica WackenforsMalin Malmsjö
Sep 30, 2000·European Journal of Pharmacology·L R WhiteJ Aasly
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Oct 19, 2013·Journal of Physiology and Biochemistry·Cristina Porras-GonzálezMaría Angeles Muñoz-Sánchez
Aug 23, 2008·Toxicological Sciences : an Official Journal of the Society of Toxicology·Cang-Bao XuLars Edvinsson
Oct 27, 2015·Toxicological Sciences : an Official Journal of the Society of Toxicology·Xue XiaoYong-xiao Cao
Jun 16, 2010·Pharmacology & Therapeutics·Cang-Bao XuLars Edvinsson
Feb 5, 2008·European Journal of Pharmacology·Evelina JohnssonLars Edvinsson
Nov 23, 2007·European Journal of Pharmacology·David NilssonMalin Malmsjö
Oct 30, 2007·European Journal of Pharmacology·David NilssonMalin Malmsjö
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May 27, 2006·European Journal of Pharmacology·Karen Eskesen, Lars Edvinsson
Jan 15, 2014·Journal of Molecular and Cellular Cardiology·Denise LauStephan Baldus

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