The endocannabinoid anandamide inhibits kinin B1 receptor sensitization through cannabinoid CB1 receptor stimulation in human umbilical vein

Eur J Pharmacol. 2009 Jan 5;602(1):176-9. doi: 10.1016/j.ejphar.2008.10.058. Epub 2008 Nov 11.


The possible inhibition of kinin B(1) receptor up-regulation by arachidonoylethanolamide (anandamide) was evaluated in isolated human umbilical vein. Anandamide and its metabolically stable analogue, R-N-(2-Hydroxy-1-methylethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide (R-(+)-methanandamide), produced a selective and dose-dependent inhibition of kinin B(1) receptor-sensitized contractile responses. The inhibitory effect of anandamide on B(1) receptor-sensitized responses failed to be modified either by 5-biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide (LY2183240), a selective anandamide uptake inhibitor, or 6-Iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-y l](4-methoxyphenyl) methanone (AM630), selective cannabinoid CB(2) receptor antagonist. However, the cannabinoid CB(1) receptor antagonist, N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophen yl)-4-methyl-1H-pyrazole-3-carboxamide (AM251), abolished anandamide effects on kinin B(1) receptor sensitization. The present results provide strong pharmacological evidence indicating that endocannabinoid anandamide inhibits kinin B(1) receptor up-regulation through cannabinoid CB(1) receptor stimulation in human umbilical vein.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arachidonic Acids / pharmacology*
  • Bradykinin B1 Receptor Antagonists*
  • Cannabinoid Receptor Modulators / pharmacology*
  • Dose-Response Relationship, Drug
  • Endocannabinoids*
  • Humans
  • Polyunsaturated Alkamides / pharmacology*
  • Receptor, Bradykinin B1 / metabolism
  • Receptor, Cannabinoid, CB1 / metabolism*
  • Umbilical Veins / drug effects*
  • Umbilical Veins / metabolism*
  • Up-Regulation


  • Arachidonic Acids
  • Bradykinin B1 Receptor Antagonists
  • Cannabinoid Receptor Modulators
  • Endocannabinoids
  • Polyunsaturated Alkamides
  • Receptor, Bradykinin B1
  • Receptor, Cannabinoid, CB1
  • anandamide