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non-intoxicative

non-psychoactive

What is CBD?  Cannabidiol (CBD) is a non-intoxicating, non-psychoactive chemical compound found in cannabis plants (e.g., hemp).  In fact, it has little binding affinity for either of the two cannabinoid receptors (CB1 and CB2), and instead modulates several non-cannabinoid receptors and ion channels. CBD is thus a pleiotropic compound producing an array of effects through multiple molecular pathways.  This is due to CBD’s unique ability to be both an agonist and an antagonist; the role it plays is dependent upon the neurotransmitter system with which it starts to interact. For example, CBD acts as an indirect antagonist of cannabinoid agonists, but acts as a 5-HT1A receptor agonist.

Neuroscience is a branch of biology that focuses on the mechanism of the human brain and understanding how the it works. The central question is how does the brain produce observed behavior. Neuroscience includes neurobiology and extends it to theoretical models, neural coding, mapping of cognitive science and psychology onto brain activity (fMRI), neural dynamics (e.g. oscillations), and models of learning, perception, and behavior. When animals are studied in neuroscience, it is as a proxy for understanding humans.  This is the field in which CBD is studied, and thus the jargon below will be utilized in explaining how CBD benefits the human body.

A receptor is a region of tissue, or a molecule in a cell membrane, that responds specifically to a particular neurotransmitter, hormone, antigen, or other substance.  An agonist is a chemical that binds to a receptor and stimulates/activates the receptor to produce a biological response.  An antagonist is a chemical that binds to a receptor and interferes with or inhibits the physiological action of another; an antagonist occupies the receptor but produces no stimulation/activation.  

5-HT1A is a member of the family of 5-HT receptors, which are activated by the neurotransmitter serotonin. Found in both the central and peripheral nervous systems, 5-HT receptors trigger various intracellular cascades of chemical messages to produce either an excitatory or inhibitory response, depending on the chemical context of the message.  At high concentrations, CBD directly activates the 5-HT1A (hydroxytryptamine) serotonin receptor, thereby conferring an anti-anxiety effect. This G-coupled protein receptor is implicated in a range of biological and neurological processes, including (but not limited to) anxiety, addiction, appetite, sleep, pain perception, nausea and vomiting.  CBDA [Cannabidiolic acid], the raw, unheated version of CBD that is present in the cannabis plant, also has a strong affinity for the 5-HT1A receptor (even more so than CBD). Preclinical studies indicate that CBDA is a potent anti-emetic, stronger than either CBD or THC, which also have anti-nausea properties.  Transient receptor potential cation channel subfamily V (i.e., TRPV1) is one of several dozen TRP (pronounced “trip”) receptor variants or subfamilies that mediate the effects of a wide range of medicinal herbs. TRPV1 has been found to mediate pain perception, inflammation and body temperature. CBD binds to TRPV1, influencing pain perception. 

 

Whereas cannabidiol directly activates the 5-HT1A serotonin receptor and several TRPV ion channels, some studies indicate that CBD functions as an antagonist that blocks, or deactivates, another G protein-coupled receptor known as GPR55.  GPR55 is involved in modulating blood pressure and bone density, among other physiological processes. Overactive GPR55 receptor signaling is associated with osteoporosis. GPR55, when activated, also promotes cancer cell proliferation and is expressed in various types of cancer. By blocking GPR55 signaling, CBD may act to decrease both bone reabsorption (which would decrease risk of osteoporosis) and cancer cell proliferation.

 

CBD also exerts an anti-cancer effect by activating PPARs [peroxisome proliferator activated receptors] that are situated on the surface of the cell’s nucleus. Activation of the receptor known as PPAR-gamma has an anti-proliferative effect as well as an ability to induce tumor regression in human lung cancer cell lines. PPAR-gamma activation degrades amyloid-beta plaque, a key molecule linked to the development of Alzheimer’s disease. This is one of the reasons why cannabidiol, a PPAR-gamma agonist, may be a useful remedy for Alzheimer’s patients. PPAR receptors also regulate genes that are involved in energy homeostasis, lipid uptake, insulin sensitivity, and other metabolic functions. Diabetics, accordingly, may benefit from a CBD-rich treatment regimen.

CBD as a reuptake inhibitor (therapeutic benefit):

Cannabidiol has a strong affinity for three kinds of FABPs, and CBD competes with our endocannabinoids, which are fatty acids, for the same transport molecules. Once it is inside the cell, anandamide is broken down by FAAH [fatty acid amide hydrolase], a metabolic enzyme, as part of its natural molecular life cycle. But CBD interferes with this process by reducing anandamide’s access to FABP transport molecules and delaying endocannabinoid passage into the cell’s interior.  CBD functions as an anandamide reuptake and breakdown inhibitor, thereby raising endocannabinoid levels in the brain’s synapses. Enhancing endocannabinod tone via reuptake inhibition may be a key mechanism whereby CBD confers neuroprotective effects against seizures, as well as many other health benefits.

CBD’s anti-inflammatory and anti-anxiety effects are in part attributable to its inhibition of adenosine reuptake. By delaying the reuptake of this neurotransmitter, CBD boosts adenosine levels in the brain, which regulates adenosine receptor activity. A1A and A2A adenosine receptors play significant roles in cardiovascular function, regulating myocardial oxygen consumption and coronary blood flow. These receptors have broad anti-inflammatory effects throughout the body.

CBD as an allosteric modulator (therapeutic benefit):

CBD also functions as an allosteric receptor modulator, which means that it can either enhance or inhibit how a receptor transmits a signal by changing the shape of the receptor.  CBD acts as a “positive allosteric modulator” of the GABA-A receptor. In other words, CBD interacts with the GABA-A receptor in a way that enhances the receptor’s binding affinity for its principal endogenous agonist, gamma-Aminobutyric acid (GABA), which is the main inhibitory neurotransmitter in the mammalian central nervous system. The sedating effects of Valium and other Benzos are mediated by GABA receptor transmission. CBD reduces anxiety by changing the shape of the GABA-A receptor in a way that amplifies the natural calming effect of GABA.

CBD has been identified as a “negative allosteric modulator” of the cannabinoid CB1 receptor, which is concentrated in the brain and central nervous system. While cannabidiol doesn’t bind to the CB1 receptor directly like THC does, CBD interacts allosterically with CB1 and changes the shape of the receptor in a way that weakens CB1’s ability to bind with THC.  As a negative allosteric modulator of the CB1 receptor, CBD lowers the ceiling on THC’s psychoactivity

 
 

Therapeutic Benefits of CBD

What is CBD?  Cannabidiol (CBD) is a non-intoxicating, non-psychoactive chemical compound found in cannabis plants (e.g., hemp).  In fact, it has little binding affinity for either of the two cannabinoid receptors (CB1 and CB2), and instead modulates several non-cannabinoid receptors and ion channels. CBD is thus a pleiotropic compound producing an array of effects through multiple molecular pathways.  This is due to CBD’s unique ability to be both an agonist and an antagonist; the role it plays is dependent upon the neurotransmitter system with which it starts to interact. For example, CBD acts as an indirect antagonist of cannabinoid agonists, but acts as a 5-HT1A receptor agonist.

Neuroscience is a branch of biology that focuses on the mechanism of the human brain and understanding how the it works. The central question is how does the brain produce observed behavior. Neuroscience includes neurobiology and extends it to theoretical models, neural coding, mapping of cognitive science and psychology onto brain activity (fMRI), neural dynamics (e.g. oscillations), and models of learning, perception, and behavior. When animals are studied in neuroscience, it is as a proxy for understanding humans.  This is the field in which CBD is studied, and thus the jargon below will be utilized in explaining how CBD benefits the human body.

A receptor is a region of tissue, or a molecule in a cell membrane, that responds specifically to a particular neurotransmitter, hormone, antigen, or other substance.  An agonist is a chemical that binds to a receptor and stimulates/activates the receptor to produce a biological response.  An antagonist is a chemical that binds to a receptor and interferes with or inhibits the physiological action of another; an antagonist occupies the receptor but produces no stimulation/activation.  

5-HT1A is a member of the family of 5-HT receptors, which are activated by the neurotransmitter serotonin. Found in both the central and peripheral nervous systems, 5-HT receptors trigger various intracellular cascades of chemical messages to produce either an excitatory or inhibitory response, depending on the chemical context of the message.  At high concentrations, CBD directly activates the 5-HT1A (hydroxytryptamine) serotonin receptor, thereby conferring an anti-anxiety effect. This G-coupled protein receptor is implicated in a range of biological and neurological processes, including (but not limited to) anxiety, addiction, appetite, sleep, pain perception, nausea and vomiting.  CBDA [Cannabidiolic acid], the raw, unheated version of CBD that is present in the cannabis plant, also has a strong affinity for the 5-HT1A receptor (even more so than CBD). Preclinical studies indicate that CBDA is a potent anti-emetic, stronger than either CBD or THC, which also have anti-nausea properties.  Transient receptor potential cation channel subfamily V (i.e., TRPV1) is one of several dozen TRP (pronounced “trip”) receptor variants or subfamilies that mediate the effects of a wide range of medicinal herbs. TRPV1 has been found to mediate pain perception, inflammation and body temperature. CBD binds to TRPV1, influencing pain perception. 

 

Whereas cannabidiol directly activates the 5-HT1A serotonin receptor and several TRPV ion channels, some studies indicate that CBD functions as an antagonist that blocks, or deactivates, another G protein-coupled receptor known as GPR55.  GPR55 is involved in modulating blood pressure and bone density, among other physiological processes. Overactive GPR55 receptor signaling is associated with osteoporosis. GPR55, when activated, also promotes cancer cell proliferation and is expressed in various types of cancer. By blocking GPR55 signaling, CBD may act to decrease both bone reabsorption (which would decrease risk of osteoporosis) and cancer cell proliferation.

 

CBD also exerts an anti-cancer effect by activating PPARs [peroxisome proliferator activated receptors] that are situated on the surface of the cell’s nucleus. Activation of the receptor known as PPAR-gamma has an anti-proliferative effect as well as an ability to induce tumor regression in human lung cancer cell lines. PPAR-gamma activation degrades amyloid-beta plaque, a key molecule linked to the development of Alzheimer’s disease. This is one of the reasons why cannabidiol, a PPAR-gamma agonist, may be a useful remedy for Alzheimer’s patients. PPAR receptors also regulate genes that are involved in energy homeostasis, lipid uptake, insulin sensitivity, and other metabolic functions. Diabetics, accordingly, may benefit from a CBD-rich treatment regimen.

 

The human endocannabinoid system

The endocannabinoid system (ECS) is a biological system composed of endocannabinoids, which are endogenous lipid-based retrograde neurotransmitters that bind to cannabinoid receptors (a type of cell membrane receptor), and cannabinoid receptor proteins that are expressed throughout the mammalian central nervous system (including the brain) and peripheral nervous system. (Notably, retrograde neurotransmission mainly serves to regulate typical, anterograde neurotransmission, rather than to actually distribute any information, supporting the case that the ECS is an important modulatory system in the function of brain, endocrine, and immune tissues.)

 

Translation of aforementioned, the endocannabinoid system is comprised of endogenous lipids (i.e., endocannabinoids), enzymes that synthesize and degrade the endocannabinoids, and cannabinoid receptors (i.e., CB1 and CB2,) and G protein-coupled receptors located in the central and peripheral nervous systems. The neurons, neural pathways, and other cells where these molecules, enzymes, and one or both cannabinoid receptor types colocalized form the endocannabinoid system.

 

The ECS is involved in regulating a variety of physiological processes and cognitive processes including appetite, pain-sensation, fertility, pregnancy, prenatal and postnatal development, as well as cognitive processes such as mood and memory.

The endocannabinoid system has been studied using genetic and pharmacological methods. These studies have revealed that cannabinoids act as neuromodulators for a variety of processes, including motor learning, appetite, and pain sensation, among other cognitive and physical processes.

 

The ECS has been recognized as an important modulatory system in the function of brain, endocrine, and immune tissues; it appears to play an important role in the secretion of hormones related to reproductive functions and response to stress.

Role in hippocampal neurogenesis.  In the adult brain, the endocannabinoid system facilitates the neurogenesis of hippocampal granule cells. Adult neurogenesis is reported to play a role in learning and memory, emotion, stress, depression, response to injury, and other conditions.

 

Energy balance and metabolism

The endocannabinoid system has been shown to have a homeostatic role by controlling several metabolic functions, such as energy storage and nutrient transport. It acts on peripheral tissues such as adipocytes, hepatocytes, the gastrointestinal tract, the skeletal muscles and the endocrine pancreas. It has also been implied in modulating insulin sensitivity. Through all of this, the endocannabinoid system may play a role in clinical conditions, such as obesity, diabetes, and atherosclerosis, which may also give it a cardiovascular role.

 

modulating the Stress response

While the secretion of glucocorticoids in response to stressful stimuli is an adaptive response necessary for an organism to respond appropriately to a stressor, persistent secretion may be harmful. The endocannabinoid system has been implicated in the habituation of the hypothalamic-pituitary-adrenal axis (HPA axis) to repeated exposure to restraint stress. Studies have demonstrated differential synthesis of anandamide and 2-AG during tonic stress. A decrease of anandamide was found along the axis that contributed to basal hypersecretion of corticosterone; in contrast, an increase of 2-AG was found in the amygdala after repeated stress, which was negatively correlated to magnitude of the corticosterone response. All effects were abolished by the CB1 antagonist AM251, supporting the conclusion that these effects were cannabinoid-receptor dependent.[53] These findings show that anandamide and 2-AG divergently regulate the HPA axis response to stress: while habituation of the stress-induced HPA axis via 2-AG prevents excessive secretion of glucocorticoids to non-threatening stimuli, the increase of basal corticosterone secretion resulting from decreased anandamide allows for a facilitated response of the HPA axis to novel stimuli.

Exploration, social behavior, and anxiety

These contrasting effects reveal the importance of the endocannabinoid system in regulating anxiety-dependent behavior. Results suggest that glutamatergic cannabinoid receptors are not only responsible for mediating aggression, but produce an anxiolytic-like function by inhibiting excessive arousal: excessive excitation produces anxiety that limited the mice from exploring both animate and inanimate objects. In contrast, GABAergic neurons appear to control an anxiogenic-like function by limiting inhibitory transmitter release. Taken together, these two sets of neurons appear to help regulate the organism's overall sense of arousal during novel situations.

Immune function

Evidence suggests that endocannabinoids may function as both neuromodulators and immunomodulators in the immune system. Here, they seem to serve an autoprotective role to ameliorate muscle spasms, inflammation, and other symptoms of multiple sclerosis and skeletal muscle spasms.[13]

Sleep

Increased endocannabinoid signaling within the central nervous system promotes sleep-inducing effects. Intercerebroventricular administration of anandamide in rats has been shown to decrease wakefulness and increase slow-wave sleep and REM sleep.[67] Administration of anandamide into the basal forebrain of rats has also been shown to increase levels of adenosine, which plays a role in promoting sleep and suppressing arousal.[68] REM sleep deprivation in rats has been demonstrated to increase CB1 receptor expression in the central nervous system.[69] Furthermore, anandamide levels possess a circadian rhythm in the rat, with levels being higher in the light phase of the day, which is when rats are usually asleep or less active, since they are nocturnal.[70]

Physical exercise

Anandamide is an endogenous cannabinoid neurotransmitter that binds to cannabinoid receptors.[6] It has been shown that aerobic exercise causes an increase in plasma anandamide levels, where the magnitude of this increase is highest at moderate exercise intensity (i.e., exercising at ~70–80% maximum heart rate).[6] Increases in plasma anandamide levels are associated with psychoactive effects because anandamide is able to cross the blood–brain barrier and act within the central nervous system.[6] Thus, because anandamide is a euphoriant and aerobic exercise is associated with euphoric effects, it has been proposed that anandamide partly mediates the short-term mood-lifting effects of exercise (e.g., the euphoria of a runner's high) via exercise-induced increases in its synthesis.[7][6]

analgesic and anxiety-reducing effects of running.

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