Characterization of G protein-coupled receptors expressed by ECV304 human endothelial cells

John Howl, Richard M. Mondszein, Mark Wheatley

Research output: Contribution to journalArticlepeer-review

10 Citations (Scopus)


The aims of this study were to characterized protein-coupled receptors endogenously expressed by ECV304 human endothelial cells, and to determine the utility of this transformed cell line as a vehicle for the expression of cloned receptors. Cellular responses to a broad range of agonists were determined by measuring changes in the intracellular content of second messengers (inositol phosphates and cyclic adenosine monophosphate). These studies identified H1 histamine receptors, P(2U)-purinoceptors and lysophosphatidic acid receptors which are functionally coupled to phosphoinositidase C. G protein-coupled receptors which bind adenosine (A2 receptor), calcitonin, and adrenaline (β-adrenoceptor), and markedly stimulate adenylyl cyclase, are also endogenously expressed by ECV304. Agonists which did not stimulate ECV304 cells are: angiotensin II, angiotensin1-7, bombesin, bradykinin, desArg9-bradykinin, carbachol, endothelin-1, neurotensin, serotonin, substance K, substance P, thrombin and vasopressin. The rat Via vasopressin receptor was expressed by lipofection in two antibiotic-resistant clonal lines and expression confirmed by measuring agonist-induced changes in inostol phosphate production. We conclude that the ECV304 cell line is a suitable in vitro system to study the signal transduction pathways of some endogenous G protein-coupled receptors known to modulate endothelial function in vivo. ECV304 is also appropriate for the expression and functional characterization of cloned receptor proteins.

Original languageEnglish
Pages (from-to)23-32
Number of pages10
JournalEndothelium: Journal of Endothelial Cell Research
Issue number1
Publication statusPublished - 1998
Externally publishedYes


  • Adrenaline
  • Calcitonin
  • Histamine
  • Lysophosphatidic acid
  • Purine
  • Vasopressin

ASJC Scopus subject areas

  • Physiology
  • Cell Biology


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