Recently, the endocannabinoid system has been recognized as an important player in brain, endocrine, and immune tissue functions. It appears that the system performs a very important role in the controlled release of the hormones involved in reproduction and stress responses. Four key elements are:

  • the endocannabinoid receptors types cannabinoid-1 and 2 (CB1 and CB2)
  • the endogenous ligands N-arachidonoylethanolamide and 2-arachidonoyl glycerol, the binder of a central metal atom to form a coordination complex
  • the enzymes involved in their synthesis and degradation
  • the cannabinoid antagonists

In humans, this system also maintains the energy levels. The endocannabinoid system controls this by influencing the function of the food intake centers of the central nervous system as well as the activity in the digestive tract. Not only does the system regulate the central and peripheral mechanisms of food intake, but also the breakdown and storage of lipids. It also maintains the turnover in the liver and adipose tissue as well as absorption and use of glucose in muscle cells.

This recent discovery leads to the speculation of future clinical use of CB1 antagonists, or blockers. Essentially, how would it do in terms of fertilization capacity or improving gonadotropin pulsatility, the reproductive hormone that is essential for establishing and maintaining early pregnancy? Can this study aid in the prevention of cardiovascular disease and type 2 diabetes?

Rimonabant is a new and selective central and peripheral CB1 blocker. It has been shown to reduce body weight and improve cardiovascular risk factor (metabolic syndrome) in obese patients by increasing high density lipoprotein (HDL)-cholesterol and adiponectin blood levels, the protein hormone involved in regulating glucose levels as well as fatty acid breakdown. Not only does it increase HDL-cholesterol, it also decreases LDL-cholesterol, leptin, and C-reactive protein (a proinflammatory marker) concentrations.

Currently, drugs that are acting as agonists of CB1 receptors (Dronabinol and Dexanabinol) are currently in favor for evaluation as treatment for neurodegenerative disorders. Other considerations have been taken into account for anxiety.

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