Document Detail


Hemodynamic effects of cannabinoids: coronary and cerebral vasodilation mediated by cannabinoid CB(1) receptors.
MedLine Citation:
PMID:  11448486     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Activation of peripheral cannabinoid CB(1) receptors elicits hypotension. Using the radioactive microsphere technique, we examined the effects of cannabinoids on systemic hemodynamics in anesthetized rats. The potent cannabinoid CB(1) receptor agonist HU-210 ([-]-11-OH-Delta(9) tetrahydrocannabinol dimethylheptyl, 10 microg/kg i.v.) reduced mean blood pressure by 57+/-5 mm Hg by decreasing cardiac index from 37+/-1 to 23+/-2 ml/min/100 g (P<0.05) without significantly affecting systemic vascular resistance index. HU-210 elicited a similar decrease in blood pressure following ganglionic blockade and vasopressin infusion. The endogenous cannabinoid anandamide (arachidonyl ethanolamide, 4 mg/kg i.v.) decreased blood pressure by 40+/-7 mm Hg by reducing systemic vascular resistance index from 3.3+/-0.1 to 2.3+/-0.1 mm Hg min/ml/100 g (P<0.05), leaving cardiac index and stroke volume index unchanged. HU-210, anandamide, and its metabolically stable analog, R-methanandamide, lowered vascular resistance primarily in the coronaries and the brain. These vasodilator effects remained unchanged when autoregulation was prevented by maintaining blood pressure through volume replacement, but were prevented by pretreatment with the cannabinoid CB(1) receptor antagonist SR141716A (N-[piperidin-1-yl]-5-[4-chlorophenyl]-1-[2,4-dichlorophenyl]-4-methyl-1H-pyrazole-3-carboxamide HCl; 3 mg/kg i.v.). Only anandamide and R-methanandamide were vasodilators in the mesentery. We conclude that cannabinoids elicit profound coronary and cerebral vasodilation in vivo by direct activation of vascular cannabinoid CB(1) receptors, rather than via autoregulation, a decrease in sympathetic tone or, in the case of anandamide, the action of a non-cannabinoid metabolite. Differences between the hemodynamic profile of various cannabinoids may reflect quantitative differences in cannabinoid CB(1) receptor expression in different tissues and/or the involvement of as-yet-unidentified receptors.
Authors:
J A Wagner; Z Járai; S Bátkai; G Kunos
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  European journal of pharmacology     Volume:  423     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  2001 Jul 
Date Detail:
Created Date:  2001-07-12     Completed Date:  2001-08-16     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  203-10     Citation Subset:  IM    
Affiliation:
Department of Pharmacology and Toxicology, Medical College of Virginia, Richmond, VA 23298, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Arachidonic Acids / pharmacology
Blood Pressure / drug effects
Brain / blood supply
Cannabinoids / antagonists & inhibitors,  pharmacology*
Coronary Circulation / drug effects
Coronary Vessels / drug effects,  physiology
Heart Rate / drug effects
Hemodynamics / drug effects*
Male
Piperidines / pharmacology
Polyunsaturated Alkamides
Pyrazoles / pharmacology
Rats
Rats, Sprague-Dawley
Receptors, Cannabinoid
Receptors, Drug / physiology
Tetrahydrocannabinol / analogs & derivatives*,  pharmacology
Vascular Resistance / drug effects
Vasodilation / drug effects
Grant Support
ID/Acronym/Agency:
R01-HL49938/HL/NHLBI NIH HHS; R01-HL59257/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/Arachidonic Acids; 0/Cannabinoids; 0/Piperidines; 0/Polyunsaturated Alkamides; 0/Pyrazoles; 0/Receptors, Cannabinoid; 0/Receptors, Drug; 112924-45-5/HU 211; 150314-39-9/methanandamide; 158681-13-1/rimonabant; 1972-08-3/Tetrahydrocannabinol; 94421-68-8/anandamide

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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