Pharmacology of Cannabinoid Receptors

Pharmacology of Cannabinoid Receptors

CB1 receptorsare found predominantly at nerve terminals where they mediate inhibition of transmitter release. CB2 receptors occur mainly on immune cells, one of their roles being to modulate cytokine release. Endogenous agonists for cannabinoid receptors also exist, and are all eicosanoids.

What is the mechanism of action of cannabinoids?

Mechanism of Action

Cannabinoids function by stimulating two receptors, cannabinoid receptor type 1 (CB1) and type 2 (CB2) within the endocannabinoid system. This system is a complex network of organs throughout the body, expressing the cannabinoid receptors and plays a homeostatic role.

What drugs bind to cannabinoid receptors?

Medicines that activate cannabinoid CB1 and CB2 receptor are already in the clinic. These are Cesamet (nabilone), Marinol (dronabinol; ?9-tetrahydrocannabinol) and Sativex (?9-tetrahydrocannabinol with cannabidiol).

What do cannabinoid receptors do?

Cannabinoid receptors have been implicated in diverse physiological and pathophysiological roles in the body, including regulation of mood, appetite, pain sensation, vascular and nonvascular smooth muscle tone, and immune function.

How do CB1 and CB2 receptors work?

CB1 and CB2 Receptors and Homeostasis. The endocannabinoid system’s most important function is to maintain homeostasis. It does this by leveraging endocannabinoids and CB1 and CB2 cannabinoid receptors in the central and peripheral nervous systems and the immune system.

What are cannabinoid drugs?

Cannabinoids are drugs that share active agents found in Cannabis (Marijuana) or were synthetically developed from those drugs. They are increasingly becoming legal, holding a potential problem for a rise in addiction for all ages.

Where are cannabinoid receptors located?

The CB1 receptors are primarily located on nerve cells in the brain, spinal cord, but they are also found in some peripheral organs and tissues such as the spleen, white blood cells, endocrine gland and parts of the reproductive, gastrointestinal and urinary tracts.

What is the difference between CB1 and CB2 receptors?

CB1 is mostly expressed in the brain, adipocytes (fat cells), hepatocytes (liver cells), and musculoskeletal tissues. Cannabinoid Receptor 2 (CB2) is associated with anti-inflammatory and immunomodulatory effects but no psychoactive effects.

What is a CB1 antagonist?

Rimonabant is a selective central cannaboid (CB1) receptor antagonist. It is an appetite suppressant in advanced development for obesity treatment. The rationale behind this drug is to reduce appetite by blocking cannaboid receptors in the hypothalamus.

What are CB1 receptor agonists?


Cannabinoid CB1 receptor agonists, including delta-9-tetra-hydrocannabinol (THC), have a wide variety of behavioral effects, including actions on motor control [13], pain [1,3], and cognitive function [47]. These drugs also have been reported to exert effects upon processes related to food intake.

What receptors are stimulated by cannabinoids?

These activate the cannabinoid 1 receptor (CB1) receptor in the central nervous system (CNS). The result can include modulation of adenylate cyclase activity to inhibit cAMP accumulation, voltage-gated calcium channels (VGCC), K+ channels and neurotransmitter release in presynaptic excitatory and inhibitory synapses.

Which of the following is characteristic of cannabinoid receptors?

Which of the following is characteristic of cannabinoid receptors? Receptor activation results in analgesia. THC is a drug that activates the cannabinoid receptors. … Receptor activation by THC reduces nausea and vomiting.

Does AEA bind to CB1?

While 2-AG is known to be a full agonist at CB1 receptors [16], AEA is a partial agonist at CB1 receptors [17] just like ?9-THC but somewhat more potent than ?9-THC in activating the CB1 receptor [1].

Does CBG bind to CB1 or CB2?

Cannabigerol (CBG) binds CB1 and CB2, but functions as a competitive antagonist for the CB1. This compound also functions as an agonist for the ?2 adrenoceptor (Cascio, Gauson, Stevenson, Ross, & Pertwee, 2010).

What type of GPCR is CB1?

Cannabinoid receptor type 1 (CB1), also known as cannabinoid receptor 1, is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene.

Cannabinoid receptor type 1.
showGene ontology
Species Human Mouse
Entrez 1268 12801

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What are cannabinoids biology?

Cannabinoids (/k??nb?n??dz? ?kn?b?n??dz/) are compounds found in cannabis. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (Delta9-THC or Delta8-THC), the primary psychoactive compound in cannabis. Cannabidiol (CBD) is another major constituent of the plant.

What are the side effects of cannabinoids?

Other effects include:
  • altered senses (for example, seeing brighter colors)
  • altered sense of time.
  • changes in mood.
  • impaired body movement.
  • difficulty with thinking and problem-solving.
  • impaired memory.
  • hallucinations (when taken in high doses)
  • delusions (when taken in high doses)

How many cannabinoids receptors are there?

Researchers have identified two cannabinoid receptors: CB1, predominantly present in the nervous system, connective tissues, gonads, glands, and organs; and CB2, predominantly found in the immune system and its associated structures. Many tissues contain both CB1 and CB2 receptors, each linked to a different action.

How many cannabinoid receptors are there in the body?

Drugs rely on knowing receptor structure

The two cannabinoid receptors, CB1 and CB2, belong to the so-called endocannabinoid system. This refers to a signaling system in the human body that regulates biological processes such as metabolism, pain sensation, neuronal activity, immune function, and so on.

Is Beta Caryophyllene a cannabinoid?

?-Caryophyllene has the distinction of being the first known dietary cannabinoid, a common component of food that has GRAS (Generally Recognized as Safe) status and is approved by the FDA for food use.

Which receptor does CBN bind to?


CBN is a weak psychoactive compound that binds the cannabinoid receptors showing higher affinity towards CB2.

What does CB1 stand for?

CB1 stands for cannabinoid receptor type 1 and is differentiated from CB2, or cannabinoid receptor type 2. While both CB1 and CB2 play key roles in your body’s endocannabinoid system, helping to regulate a broad range of bodily functions and effects, CB1 is expressed primarily in the brain, central nervous system, …

What happens if you block the CB1 receptor?

It has been recently demonstrated that a cannabinoid CB1 receptor neutral antagonist AM4113 can produce suppression of food intake and food-reinforced behavior in animals (Sink et al., 2008), without producing some unwanted side effects such as nausea and vomiting (Sink et al., 2008), (the main side effects in terms of …

What is an agonist?

Listen to pronunciation. (A-guh-nist) A drug or substance that binds to a receptor inside a cell or on its surface and causes the same action as the substance that normally binds to the receptor.

What are cannabinoid agonists?

The active compounds tetrahydrocannabinol (THC), cannabidiol, cannabinol, and tetrahydrocannabivarin in the plant C. sativa are physiological and psychoactive compounds. These active compounds are cannabinoid receptor agonists, meaning they stimulate the cannabinoid receptor to enhance its effect.

Does your brain have cannabinoid receptors?

The endogenous cannabinoid systemnamed for the plant that led to its discoveryis one of the most important physiologic systems involved in establishing and maintaining human health. Endocannabinoids and their receptors are found throughout the body: in the brain, organs, connective tissues, glands, and immune cells.

What neurotransmitters facilitate learning?

Dopamine is a pleasure chemical and GABA is a learning neurotransmitter.

Is anandamide a CB1 receptor?

Physiological functions

Anandamide’s effects can occur in either the central or peripheral nervous system. These distinct effects are mediated primarily by CB1 cannabinoid receptors in the central nervous system, and CB2 cannabinoid receptors in the periphery.

What kind of receptor is CB1?

The cannabinoid type 1 receptor (CB1) is a presynaptically localized Gi/o-coupled receptor that is among the most abundant G proteincoupled receptors in the central nervous system.

What is CBC in hemp?

Cannabichromene, also known as CBC, is classified as one of the ‘big six’ of cannabinoids, the 6 most researched cannabinoids of the cannabis sativa plant. CBC has the same origins as CBD in that it converts from CBGA into CBCA and then into CBC after exposure to ultraviolet light or heat.

Does CBG bind to receptors?

According to recent research, CBG binds with both the CB1 and CB2 receptors. This indicates that CBG has a greater potential efficacy than cannabinoids that bind with only one receptor type.

Is Delta 8 a CBG?

While CBG is non-psychoactive, Delta-8-THC is. Delta-8-THC is an analog of Delta-9-tetrahydrocannabinol (THC), which means it has a similar structure, and similar effects to THC. However, Delta-8-THC has some key differences from THC that are important to consider.

What is the chemical formula of cannabinoids?

Tetrahydrocannabinol (THC) is the principal psychoactive constituent of cannabis and one of at least 113 total cannabinoids identified on the plant.

Clinical data
ECHA InfoCard 100.153.676
Chemical and physical data
Formula C21H30O2
Molar mass 314.469 gmol?1

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What plants produce cannabinoids?

Until recently, scientists had identified cannabinoids only in the Cannabis plant, commonly called marijuana or hemp. Current research, however, has found cannabinoids in many plants, including clove, black pepper, Echinacea, broccoli, ginseng, and carrots.

Are cannabinoids alkaloids?

As discussed earlier, THC, a cannabinoid, is not an alkaloid. It does not form salts in an aqueous solution (i.e., it’s not soluble in water). Rather, THC is an oily substance; it is non-polar and extremely lipid soluble (lipophilic).

What is a Schedule 1 drug?

Schedule I drugs, substances, or chemicals are defined as drugs with no currently accepted medical use and a high potential for abuse. Some examples of Schedule I drugs are: heroin, lysergic acid diethylamide (LSD), marijuana (cannabis), 3,4-methylenedioxymethamphetamine (ecstasy), methaqualone, and peyote.

Is copaiba a CBD?

What is CBD? There’s some distinct differences between CBD and between Copaiba essential oil that I keep referring to it as CBD and Copaiba essential oil because in fact Copaiba is an essential oil where CBD is not an essential oil. It is a botanical; it’s an isolated molecule.

What is limonene terpene?

Limonene is an aromatic cannabis terpene produced in the flower’s resin glands. In isolation, it’s commonly associated with fruity, citrus aromas, and it’s found in many everyday items like fruit rinds, cosmetics, and cleaning products.

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