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How the world got lost on
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May 10, 2009: by Bill Sardi
Something rather remarkable is happening in biological research. It involves study of reward centers in the brain and it spells promise for people who wish to overcome unhealthy habits such as tobacco use, alcohol over-consumption, dependency upon street drugs and even overeating.
A short course in how molecules affect the brain-reward centers is in order.
Brain cells have protein molecules on their surface (the plasma membrane) to which another molecule can be attached. This is called a cell receptor site. Molecules that attach to cell receptors are called ligands. Some of these ligands are hormones, nerve-transmitters (neurotransmitters), toxins, viruses, drugs, and molecules found in the diet.
Some molecules have greater affinity to brain cell receptor sites than others. A molecular ligand that fully or partially activates the cell receptor is called an agonist. Molecules that bind to the receptors but don’t activate them are called cell receptor antagonists. They block other molecules that can activate the receptor.
There, you now have completed a short course in cell receptors. Recognize most modern drugs work by activation or inactivation of cell receptor sites.
A widely studied receptor site is the cannibinoid receptor. Cannibinoids are molecules that are made inside the body or acquired from the diet, or consumed as a drug. The best known cannabinoid molecules are obtained from the cannabis plant – more commonly known as the street drug marijuana, hashish or “pot.”
Tetrahydrocannabinol (THC) is the primary psychoactive component of the plant. Medically, it appears to ease moderate pain and preserves brain function.
THC and marijuana is known to produce dependence, but also produces lean bodies. Appetite is suppressed by the ability of THC to block the cannabinoid 1 (CB1) brain cell receptor site.
Today Americans use the Acomplia (rimonabant), an FDA-approved appetite suppressant and weight loss drug that blocks the cannabinoid 1 cell receptor. However, there are side effects produced by this drug, which include depression, anxiety and nausea. About 1 in 8 patients taking Acomplia are unable to continue due to side effects. Marijuana has its well-known side effects, including interruption of emotional development, short-term memory loss and an overly-placid personality.
Ken Mackie, researcher at the University of Washington, School of Medicine, in a landmark report entitled “Cannabinoid Receptors As Therapeutic Targets,” points to cannabinoid receptor blockers as potential therapy of drug addiction, alcohol abuse, smoking habituation and overeating disorders. [Annual Review Pharmacology Toxicology 2006. 46:101–22]
Remarkably, in 2006 researchers at McGill University report that there are binding sites (cell receptor sites) that exhibit strong binding to small molecules in red wine, including resveratrol (rez-vair-ah-trawl). The exciting discovery of the existence of a resveratrol binding site in brain cells has been overlooked. Molecules in green tea called catechins and resveratrol in red wine were found to be strongly bound to brain cell receptor sites. [Journal Pharmacology Experimental Therapeutics 2006 July; 318(1):238-45]
More recently, researchers at the Department of Pharmacology and Toxicology
College of Medicine at the University of Arkansas for Medical Sciences report that resveratrol selectively binds to the CB1 cannabinoid cell receptor even at very low concentration and could serve as a potent anti-drug dependency or anti-obesity agent. [Journal Pharmacology Experimental Therapeutics, April 9, 2009]
Resveratrol is reported to elevate mood, improve mental performance, and produce long-term weight control among some users of dietary supplements. In fact, resveratrol has been shown to mimic the effects of anti-depressant drugs (MAO inhibitors). [Biochemical Biophysical Research Communications 2006 Jun 2; 344(2):688-95]
Mega-dose resveratrol has been reported to produce symptoms of anxiety and nausea similar to those produced by rimonabant (Acomplia). [Cancer Epidemiology Biomarkers Prevention 2007 Jun; 16(6):1246-52] Modest doses are suggested for those who wish to self experiment.
Weight control properties of resveratrol have been found to be heightened by the accompaniment of quercetin, green tea molecules and vitamin D. [Journal Medicinal Food. 2008 Dec; 11(4):773-83; Life Science 2008 May 7; 82(19-20):1032-9; Life Science 2008 May 7;82(19-20):1032-9]
Wanna get naturally high? Try resveratrol. It is modern molecular medicine to the nth degree, and it comes without the dependency, jail time or other side effects associated with smoking weed. ####
© 2009 Bill Sardi. Not for posting at other websites. Violators will be prosecuted.