Cannabinoid Receptor Structure Revealed - Breakthrough - 2016
Cannabinoid Receptor Science
"The expression of these CB1 receptors is believed to prevent the development of excessive neuronal activity, reducing pain and other inflammatory symptoms. "
The primary structure the CB1 Cannabinoid Receptor was revealed for the first time in 2016. This pioneering research was funded by the National Institute for Drug Abuse (NIDA) and National Institute of Health.
The CB1 receptor - found in most of the body's cells - modulates neurotransmitter release when activated by cannabinoids. Cannabinoids are generated naturally inside the body (endocannabinoids) or are introduced into the body as cannabis or synthetic marijuana. For example, THC, the main psychoactive ingredient is known to bind with the CB1 receptor to produce its many medicinal and cerebral-psychoactive effects.
CB1 receptors have been identified on the cells of the pituitary gland, thyroid gland, and possibly in the adrenal gland. CB1 is also expressed in several cells governing metabolism; fat, muscle, liver, kidney, lungs, endothelial , Kupffer and stellate cells of the liver, and are abundant in the digestive tract. CB1 is present in Leydig cells, in sperm, ovaries, oviducts myometrium, decidua, and placenta. CB1 furntion has also been implicated in the proper development of the embryo. The expression of these receptors is believed to prevent the development of excessive neuronal activity, reducing pain and other inflammatory symptoms.
While this new model and diagram look convincing enough, the actual structural details of the CB1 and CB2 receptors are very foggy. These new findings will likely go a long way to understanding the details, how cannabis works so well to treat a great number of diseases and symptoms. The cannabinoids of marijuana are well known to modulate the CB1 receptor and this effect is used to treat a variety of conditions including chronic pain, inflammation of all kinds, obesity, anorexia, nervous disorders and even substance abuse and behavioral problems.
"Cannabinoids can produce very different outcomes, depending on how they bind to the CB1 receptor, by understanding how these chemicals bind to the CB1 receptor will help guide the design of new medications and provide insight into the therapeutic promise of the body's cannabinoid system." - Nora D. Volkow, M.D.
Resolution of the binding pocket provides a route for logical CB1 drug design. Researchers found that a molecule (AM 6538), inactivated and crystallized at the CB1 receptor.
The various molecules that activate the CB1 receptor.
The three-dimensional structure of the CB1-AM6538 complex was determined using x-ray crystallography, which infers molecular shape by measuring the angles of x-rays as they interact with the crystal structure. Using assumptions from previous evidence of chemical action, researchers predicted how cannabinoids fit into a 3D CB1 model. They also calculates the resident time each cannabinoid bound to the CB1 receptor, providing a mechanism to explain why different molecules longer and shorter-lasting effects.
"We found that the CB1 receptor consists of multiple sub-pockets and channels, this complex structure will allow chemists to design diverse compounds that specifically target portions of the receptor to produce desired effects." - Alexandros Makriyannis, Director - Center for Drug Discovery, NEU of Boston
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"This new description of the receptor's structure will likely provide a better insight into how natural and synthetic cannabinoids work at the cellular level." MMJDoctorOnline Science
Tian Hua et al. Crystal Structure of the Human Cannabinoid Receptor CB1 Journal Cell, 2016; DOI: https://dx.doi.org/10.1016/j.cell.2016.10.004
Possible Efficacy Related Differences Among Cannabinoid Agonists Here, we show that the efficacy of two CB agonists - Δ9-tetrahydrocannabinol (THC) and the 3- adamantyl CB - can be differentiated with CB antagonists.
CB1 receptor - slice from the larger protein. Cannabinoids fit in here and start the chain reaction ......