The Endocannabinoid System

Boyd, Steven T.

doi:10.1592/phco.26.12part2.218s

Cited by 36 publications

(36 citation statements)

References 26 publications

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“…The CB 1 receptor is expressed primarily in the central nervous system (2), whereas the CB 2 receptor is expressed in immune cells (3), although recent studies have described the presence of detectable levels of CB 2 receptors in brain-stem neurons (4) and the spinal cord (5). These receptors are activated by endogenous ligands derived from membrane lipids termed ''endocannabinoids'' (6)(7)(8). Recent studies have proposed important roles for the endocannabinoid system (consisting of the receptors and endogenous ligands) in many physiological and pathophysiological processes.…”

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confidence: 99%

“…Recent studies have proposed important roles for the endocannabinoid system (consisting of the receptors and endogenous ligands) in many physiological and pathophysiological processes. Thus, the development of agonists and antagonists, including those with marked selectivity for CB 1 or CB 2 receptors, is the focus of intense research (6)(7)(8).…”

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confidence: 99%

“…These include Parkinson's disease, Alzheimer's disease, major depression, inflammation, neuropathic pain, and obesity (6,8,9). Because the endocannabinoid system is involved in a wide array of diseases that are of epidemiological relevance to the developed world, compounds that modulate cannabinoid receptors are good targets for the development of drugs that could be useful in the treatment of such diseases.…”

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confidence: 99%

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Hemopressin is an inverse agonist of CB ₁ cannabinoid receptors

Heimann

Gomes

Dale

et al. 2007

Proc. Natl. Acad. Sci. U.S.A.

226

240

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To date, the endogenous ligands described for cannabinoid receptors have been derived from membrane lipids. To identify a peptide ligand for CB 1 cannabinoid receptors, we used the recently described conformation-state sensitive antibodies and screened a panel of endogenous peptides from rodent brain or adipose tissue. This led to the identification of hemopressin (PVNFKFLSH) as a peptide ligand that selectively binds CB 1 cannabinoid receptors. We find that hemopressin is a CB 1 receptor-selective antagonist, because it is able to efficiently block signaling by CB 1 receptors but not by other members of family A G protein-coupled receptors (including the closely related CB2 receptors). Hemopressin also behaves as an inverse agonist of CB 1 receptors, because it is able to block the constitutive activity of these receptors to the same extent as its well characterized antagonist, rimonabant. Finally, we examine the activity of hemopressin in vivo using different models of pain and find that it exhibits antinociceptive effects when administered by either intrathecal, intraplantar, or oral routes, underscoring hemopressin's therapeutic potential. These results represent a demonstration of a peptide ligand for CB 1 cannabinoid receptors that also exhibits analgesic properties. These findings are likely to have a profound impact on the development of novel therapeutics targeting CB 1 receptors.

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confidence: 99%

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confidence: 99%

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Hemopressin is an inverse agonist of CB ₁ cannabinoid receptors

Heimann

Gomes

Dale

et al. 2007

Proc. Natl. Acad. Sci. U.S.A.

226

240

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“…The endocannabinoid system, for instance, is an important regulator for all of those functions (Boyd, 2006;Pagotto et al, 2006). Elevated levels of the endogenous cannabinoids (anandamide and 2-arachidonoyl-glycerol) have been found in obese individuals (Engeli et al, 2005;Osei-Hyiaman et al, 2005, 2006 and correlate with intra-abdominal adiposity (Cote et al, 2007).…”

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confidence: 99%

The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the Expression of Phosphatidylinositol-3-kinase

Esposito

Proto²,

Gazzerro³

et al. 2008

Molecular Pharmacology

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The endocannabinoid system regulates food intake, energy, and glucose metabolism at both central and peripheral levels. We have investigated the mechanism by which it may control glucose uptake in skeletal muscle cells. Detectable levels of the cannabinoid receptor type 1 (CB1) were revealed in L6 cells. Exposure of differentiated L6 myotubes to the CB1 antagonist rimonabant (SR141716) selectively increased 2-deoxyglucose uptake (2-DG) in a time-and dose-dependent manner. A similar effect was induced by genetic silencing of CB1 by small interfering RNA. Protein expression profiling revealed that both the regulatory p85 and the catalytic p110 subunits of the phosphatidylinositol-3-kinase (PI3K) were increased by SR141716. No significant change in the cellular content of other known molecules regulating PI3K was observed. However, phosphoinositidedependent kinase-1, Akt/protein kinase B, and protein kinase C activities were rapidly induced after SR141716 treatment of L6 cells in a PI3K-dependent manner. The stimulatory effect of SR141716 on PI3K expression and activity was largely prevented by

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“…The ECS plays a role in regulation of appetite and metabolism [18]. Modulation of the ECS affects the four core attributes of MetS [19].…”

Section: Discussionmentioning

confidence: 99%

Relationship between Years of Marijuana Use and the Four Main Diagnostic Criteria for Metabolic Syndrome among United States Adults

Yankey¹,

Rothenberg²,

Strasser³

et al. 2017

J Addict Res Ther

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Objective: Research on marijuana use suggests a protective effect on metabolic syndrome. National Cholesterol Education Program, Adult Treatment Panel III, World Health Organization, European Group for the study of Insulin Resistance and International Diabetes Federation have different criteria for metabolic syndrome. Definitions of both marijuana use and criteria for metabolic syndrome may influence the observed effects. We examine the relationship of years of marijuana use with the four common definitions of metabolic syndrome.Method: This is a cross-sectional study of 3051 adults aged ≥ 20 years who participated in the National Health and Nutrition Examination Survey 2011-2012. Only participants who responded to the question, "Have you ever even once used marijuana or hashish?" were enrolled. Using multivariate logistic regression, we estimated odds ratios for metabolic syndrome with each year of marijuana use.Results: Adjusted odds ratios (AOR) for having metabolic syndrome with each increase in year of marijuana use was 1.05 (95% CI: 1.02, 1.08) using National Cholesterol Education Program Adult Treatment Panel III (ATP III) criteria. Respective AOR using International Diabetes Federation (IDF) was 1.08 (95% CI: 1.04, 1.13) and 1.05 (95% CI: 1.04, 1.13) using World Health Organization (WHO) or European Group for the study of Insulin Resistance (EGIR) criteria. Using ATP III or IDF criteria, the adjusted odds ratio of having hypertension (AOR Hyp) for each year of marijuana use was 1.07 (95% CI: 1.03, 1.12). Using WHO criteria, AOR Hyp was 1.05 (95% CI: 1.01, 1.09) and 1.08 (95% CI: 1.03, 1.12) using EGIR. All the applicable criteria show increased odds for abdominal obesity: AOR 1.06 (95% CI: 1.00, 1.11) (ATP III), 1.09 (95% CI: 1.05, 1.14) (EGIR) or 1.07 (95% CI: 1.01, 1.13) (IDF). Adjusted odds ratio for having high oral glucose tolerance test levels was 1.12 (95% CI: 1.07, 1.18) using WHO and EGIR criteria. Conclusion:Irrespective of the criteria for metabolic syndrome, each year of marijuana use showed increased odds of having metabolic syndrome, hypertension or high oral glucose tolerance test levels. This increased odd is in contrast to most findings in literature. The small, yet consistent increase in odds for hypertension was slightly higher than that observed with cigarette smoking. Recreational marijuana use may be detrimental to cardiovascular health. A standardized definition of marijuana use will be relevant for further investigation.

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The Endocannabinoid System

Cited by 36 publications

References 26 publications

Hemopressin is an inverse agonist of CB ₁ cannabinoid receptors

Hemopressin is an inverse agonist of CB ₁ cannabinoid receptors

The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the Expression of Phosphatidylinositol-3-kinase

Relationship between Years of Marijuana Use and the Four Main Diagnostic Criteria for Metabolic Syndrome among United States Adults

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The Endocannabinoid System

Cited by 36 publications

References 26 publications

Hemopressin is an inverse agonist of CB 1 cannabinoid receptors

Hemopressin is an inverse agonist of CB 1 cannabinoid receptors

The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the Expression of Phosphatidylinositol-3-kinase

Relationship between Years of Marijuana Use and the Four Main Diagnostic Criteria for Metabolic Syndrome among United States Adults

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Hemopressin is an inverse agonist of CB ₁ cannabinoid receptors

Hemopressin is an inverse agonist of CB ₁ cannabinoid receptors