Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid receptors are of a class of cell membrane receptors under the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids, produced by the mammillary body; plant cannabinoids (such as Cannabidiol, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). All of the endocannabinoids and plant cannabinoids are lipophilic, such as fat soluble compounds.

An Overview of Cannabinoid Receptor

Cannabinoid (CB) Receptor is a receptor that is responsive to hemp, such as C9-THC. Cannabinoid receptor is a G protein-coupled receptor, which can inhibit the activity of adenylate cyclase and decrease the level of intracellular cyclic adenylate by inhibiting G protein. Cannabinoid receptors can also regulate ion channels, resulting in reducing the release of neurotransmitters in presynaptic membrane neurons, thus making the postsynaptic membrane produce corresponding excitatory or inhibitory effects, which is the basis of the endogenous cannabinoid system. In addition, CB receptor can activate multiple intracellular signal transduction pathways.

Major types of Cannabinoid Receptor

CB1R and CB2R are two kinds of CB receptor subtypes. CB1R have been identified as receptors identified by autoradiography and radioligand binding studies using tritium labeled CP55940. It consists of 473 amino acids and 17 transmembrane regions. CB2R contains 360 amino acids. CB1R is mainly present in the central nervous system. CB2Rs are mainly found in peripheral neurons, and one of their functions is to block the release of neurotransmitters. Their main area difference is amino acid sequences, which results their signal transduction mechanisms, organ distribution, and sensitivity to certain agonists and inhibitors is different.

Inhibition of Cannabinoid Receptor

Because CB1R inhibitors act directly on the central nervous system, the activity is also diverse. Typical CB1R inhibitors such as diarylpyrazole, which is a highly efficient CB1R selective ligand. SR141716 developed by Sanofi, can quickly block or reverse the regulatory effects of CB1R and selectively bind to CB1R. The two analogues of SR141716, AM251 and AM281, also blocked the affinity of CB1R. AM281 has 350 times more affinity to CB1R than CB2R and had higher selectivity.

Cannabinoid Receptorand diseases

At present, cannabinoids are mainly used as adjuvant in anti-tumor therapy and used to relieve pain symptoms. In recent years, a number of studies have shown that cannabinoids have a significant inhibitory effect on breast cancer, prostate cancer, glioma, leukemia, lung cancer, skin cancer, thyroid cancer and pancreatic cancer. The anti-tumor effect of cannabinoids varies according to tissue type and its mechanism is different. Many pathways can be affected simultaneously.

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