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Enhanced G-protein coupled receptors-mediated contraction and reduced endothelium-dependent relaxation in hypertension

Li, He; Cao, Yong-Xiao; Liu, Hao and Xu, Cang-Bao LU (2007) In European Journal of Pharmacology 557(2-3). p.186-194
Abstract
The present study was designed to demonstrate a hypothesis that some G-protein coupled receptors are up-regulated and a dysfunction of endothelium occurs in hypertension. The arteries from hypertensive patients and spontaneously hypertensive rats (SHR) were tested. An in vitro myograph system was used to obtain concentration-contraction curves mediated by endothelin ETA, endothelin ETB, 5-hydroxytryptamine 2A (5HT(2A))-receptors and alpha(1)-adrenoceptors in the arterial segments. In hypertensive patients, the maximum contractions (E-max) induced by endothelin ETB, endothelin ETA and 5-HT receptors were significantly increased with elevated pEC(50) values, while a significantly leftward shift of alpha(1)-adrenoceptor-mediated contraction... (More)
The present study was designed to demonstrate a hypothesis that some G-protein coupled receptors are up-regulated and a dysfunction of endothelium occurs in hypertension. The arteries from hypertensive patients and spontaneously hypertensive rats (SHR) were tested. An in vitro myograph system was used to obtain concentration-contraction curves mediated by endothelin ETA, endothelin ETB, 5-hydroxytryptamine 2A (5HT(2A))-receptors and alpha(1)-adrenoceptors in the arterial segments. In hypertensive patients, the maximum contractions (E-max) induced by endothelin ETB, endothelin ETA and 5-HT receptors were significantly increased with elevated pEC(50) values, while a significantly leftward shift of alpha(1)-adrenoceptor-mediated contraction was seen. Similar results were obtained in SHR. Specific antagonists for 5-HT2A receptors or alpha(1)-adrenoceptors rightward shifted the concentration-contractile curves induced by 5-HT or noradrenalin, while the Emax were not significantly altered, suggesting that the contractions were mediated by 5-HT2A receptors and ocl-adrenoceptors, respectively. Endothelium-dependent maximum relaxation (R-max) in the arterial segments induced by acetylcholine was significantly decreased in both hypertensive patients and SHR. In addition, nitric oxide- and endothelium-derived hyperpolarizing factor-mediated dilatations were decreased significantly and the arterial enclothelial cells were in part lost in SHR. In conclusion, endotheliD ETB, endothelin ETA, 5-HT2A receptor- and alpha-adrenoceptor-mediated contractions were increased in hypertension, while the endotheliurn and its ftinctions were damaged. (c) 2006 Elsevier B.V All rights reserved. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
endothelin receptor, 5-HT receptor, endothelium, alpha(1)-adrenoceptor, hypertension
in
European Journal of Pharmacology
volume
557
issue
2-3
pages
186 - 194
publisher
Elsevier
external identifiers
  • wos:000244494400015
  • scopus:33846821685
ISSN
1879-0712
DOI
10.1016/j.ejphar.2006.11.057
language
English
LU publication?
yes
id
cb976cef-3f0b-4236-8326-b8803bbb99ff (old id 673751)
date added to LUP
2007-12-12 14:08:51
date last changed
2017-10-01 03:35:30
@article{cb976cef-3f0b-4236-8326-b8803bbb99ff,
  abstract     = {The present study was designed to demonstrate a hypothesis that some G-protein coupled receptors are up-regulated and a dysfunction of endothelium occurs in hypertension. The arteries from hypertensive patients and spontaneously hypertensive rats (SHR) were tested. An in vitro myograph system was used to obtain concentration-contraction curves mediated by endothelin ETA, endothelin ETB, 5-hydroxytryptamine 2A (5HT(2A))-receptors and alpha(1)-adrenoceptors in the arterial segments. In hypertensive patients, the maximum contractions (E-max) induced by endothelin ETB, endothelin ETA and 5-HT receptors were significantly increased with elevated pEC(50) values, while a significantly leftward shift of alpha(1)-adrenoceptor-mediated contraction was seen. Similar results were obtained in SHR. Specific antagonists for 5-HT2A receptors or alpha(1)-adrenoceptors rightward shifted the concentration-contractile curves induced by 5-HT or noradrenalin, while the Emax were not significantly altered, suggesting that the contractions were mediated by 5-HT2A receptors and ocl-adrenoceptors, respectively. Endothelium-dependent maximum relaxation (R-max) in the arterial segments induced by acetylcholine was significantly decreased in both hypertensive patients and SHR. In addition, nitric oxide- and endothelium-derived hyperpolarizing factor-mediated dilatations were decreased significantly and the arterial enclothelial cells were in part lost in SHR. In conclusion, endotheliD ETB, endothelin ETA, 5-HT2A receptor- and alpha-adrenoceptor-mediated contractions were increased in hypertension, while the endotheliurn and its ftinctions were damaged. (c) 2006 Elsevier B.V All rights reserved.},
  author       = {Li, He and Cao, Yong-Xiao and Liu, Hao and Xu, Cang-Bao},
  issn         = {1879-0712},
  keyword      = {endothelin receptor,5-HT receptor,endothelium,alpha(1)-adrenoceptor,hypertension},
  language     = {eng},
  number       = {2-3},
  pages        = {186--194},
  publisher    = {Elsevier},
  series       = {European Journal of Pharmacology},
  title        = {Enhanced G-protein coupled receptors-mediated contraction and reduced endothelium-dependent relaxation in hypertension},
  url          = {http://dx.doi.org/10.1016/j.ejphar.2006.11.057},
  volume       = {557},
  year         = {2007},
}