Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunities

The long history of Cannabis sativa had its development stimulated and oriented for medicine after the discovery and chemical characterization of its main active ingredient, the 9-tetrahydrocannabinol (9-THC). Consequently, a binding site for 9-THC was identified in rat brains and the first cannabin...

Full description

Bibliographic Details
Main Authors: Pedro Cunha, Ana M Romão, Filipa Mascarenhas-Melo, Helena M Teixeira, Flávio Reis
Format: Article
Language:English
Published: Wolters Kluwer Medknow Publications 2011-01-01
Series:Journal of Pharmacy and Bioallied Sciences
Subjects:
Online Access:http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2011;volume=3;issue=3;spage=350;epage=360;aulast=Cunha
_version_ 1811202491519336448
author Pedro Cunha
Ana M Romão
Filipa Mascarenhas-Melo
Helena M Teixeira
Flávio Reis
author_facet Pedro Cunha
Ana M Romão
Filipa Mascarenhas-Melo
Helena M Teixeira
Flávio Reis
author_sort Pedro Cunha
collection DOAJ
description The long history of Cannabis sativa had its development stimulated and oriented for medicine after the discovery and chemical characterization of its main active ingredient, the 9-tetrahydrocannabinol (9-THC). Consequently, a binding site for 9-THC was identified in rat brains and the first cannabinoid receptor (CB1) was cloned, followed by the CB2 and by the discover of two endogenous agonists: anandamide and 2-arachidonoyl glycerol. Cannabinoid receptors, endocannabinoids and the enzymes that catalyze its synthesis and degradation constitute the endocannabinoid system (ECS), which plays an important role in the cardiovascular system. In vivo experiments with rats have demonstrated the action of anandamide and 2-AG on the development of atherosclerotic plaque, as well as an effect on heart rate, blood pressure, vasoactivity and energy metabolism (action in dyslipidemia and obesity). Recent studies with an antagonist of CB1 receptors showed that the modulation of ECS can play an important role in reducing cardiovascular risk in obese and dyslipidemic patients. Similarly, studies in rats have demonstrated the action of CB2 receptors in adhesion, migration, proliferation and function of immune cells involved in the atherosclerotic plaque formation process. The evidence so far gathered shows that the modulation of ECS (as agonism or antagonism of its receptors) is an enormous potential field for research and intervention in multiple areas of human pathophysiology. The development of selective drugs for the CB1 and CB2 receptors may open a door to new therapeutic regimens.This review article aims to address the key findings and evidences on the modulation of ECS, in order to prospect future forms of therapeutic intervention at the cardiovascular level. A recent, emerging, controversial and of undoubted scientific interest subject, which states as a potential therapeutic target to reach in the 21 st century.
first_indexed 2024-04-12T02:40:13Z
format Article
id doaj.art-da455bf16ebb4cb3b41728b3d0b78d52
institution Directory Open Access Journal
issn 0975-7406
0976-4879
language English
last_indexed 2024-04-12T02:40:13Z
publishDate 2011-01-01
publisher Wolters Kluwer Medknow Publications
record_format Article
series Journal of Pharmacy and Bioallied Sciences
spelling doaj.art-da455bf16ebb4cb3b41728b3d0b78d522022-12-22T03:51:20ZengWolters Kluwer Medknow PublicationsJournal of Pharmacy and Bioallied Sciences0975-74060976-48792011-01-013335036010.4103/0975-7406.84435Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunitiesPedro CunhaAna M RomãoFilipa Mascarenhas-MeloHelena M TeixeiraFlávio ReisThe long history of Cannabis sativa had its development stimulated and oriented for medicine after the discovery and chemical characterization of its main active ingredient, the 9-tetrahydrocannabinol (9-THC). Consequently, a binding site for 9-THC was identified in rat brains and the first cannabinoid receptor (CB1) was cloned, followed by the CB2 and by the discover of two endogenous agonists: anandamide and 2-arachidonoyl glycerol. Cannabinoid receptors, endocannabinoids and the enzymes that catalyze its synthesis and degradation constitute the endocannabinoid system (ECS), which plays an important role in the cardiovascular system. In vivo experiments with rats have demonstrated the action of anandamide and 2-AG on the development of atherosclerotic plaque, as well as an effect on heart rate, blood pressure, vasoactivity and energy metabolism (action in dyslipidemia and obesity). Recent studies with an antagonist of CB1 receptors showed that the modulation of ECS can play an important role in reducing cardiovascular risk in obese and dyslipidemic patients. Similarly, studies in rats have demonstrated the action of CB2 receptors in adhesion, migration, proliferation and function of immune cells involved in the atherosclerotic plaque formation process. The evidence so far gathered shows that the modulation of ECS (as agonism or antagonism of its receptors) is an enormous potential field for research and intervention in multiple areas of human pathophysiology. The development of selective drugs for the CB1 and CB2 receptors may open a door to new therapeutic regimens.This review article aims to address the key findings and evidences on the modulation of ECS, in order to prospect future forms of therapeutic intervention at the cardiovascular level. A recent, emerging, controversial and of undoubted scientific interest subject, which states as a potential therapeutic target to reach in the 21 st century.http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2011;volume=3;issue=3;spage=350;epage=360;aulast=CunhaAtherosclerosiscannabinoidscardiovascular systemendocannabinoidshypertensionshockischemia/reperfusiontherapeutics
spellingShingle Pedro Cunha
Ana M Romão
Filipa Mascarenhas-Melo
Helena M Teixeira
Flávio Reis
Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunities
Journal of Pharmacy and Bioallied Sciences
Atherosclerosis
cannabinoids
cardiovascular system
endocannabinoids
hypertension
shock
ischemia/reperfusion
therapeutics
title Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunities
title_full Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunities
title_fullStr Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunities
title_full_unstemmed Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunities
title_short Endocannabinoid system in cardiovascular disorders - new pharmacotherapeutic opportunities
title_sort endocannabinoid system in cardiovascular disorders new pharmacotherapeutic opportunities
topic Atherosclerosis
cannabinoids
cardiovascular system
endocannabinoids
hypertension
shock
ischemia/reperfusion
therapeutics
url http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2011;volume=3;issue=3;spage=350;epage=360;aulast=Cunha
work_keys_str_mv AT pedrocunha endocannabinoidsystemincardiovasculardisordersnewpharmacotherapeuticopportunities
AT anamromao endocannabinoidsystemincardiovasculardisordersnewpharmacotherapeuticopportunities
AT filipamascarenhasmelo endocannabinoidsystemincardiovasculardisordersnewpharmacotherapeuticopportunities
AT helenamteixeira endocannabinoidsystemincardiovasculardisordersnewpharmacotherapeuticopportunities
AT flavioreis endocannabinoidsystemincardiovasculardisordersnewpharmacotherapeuticopportunities