A Brief Introduction to CB-2

The endocannabinoid system is a critical physiological system, serving as a broad spectrum modulator involved in regulating multiple physiological activities, cognitive processes, and pharmacological effects of cannabis. The endocannabinoid system widely distributes throughout the human body that functions to maintain the homeostasis of the body. In the central nervous system (CNS), the endocannabinoid system exerts fundamental roles in neuronal development, brain plasticity, emotions, learning, memory, etc., all of which make the endocannabinoid system a potential key target for the treatment of neurological diseases, especially for psychiatric disorders.

The cannabinoid receptor is an indispensable member of the endocannabinoid system, which is responsible for binding to cannabinoid ligands and mediates multiple signal pathways. Two cannabinoid receptors have been identified, cannabinoid receptors type 1 (CB-1) and cannabinoid receptors type 2 (CB-2). Compared with CB-1 that is highly expressed in the CNS, CB-2 is more limited to distribution in the immune system and peripheral tissues, and less in the brain. Similar to CB-1, CB-2 is a type of G protein-coupled receptor and coupled to pertussis toxin (PTX)-sensitive Gi/o protein. By coupling to different Gi/o proteins, CB-2 mediates an array of signaling transduction pathways when activated by agonist ligands, including adenylyl cyclase, MAPK-ERK pathway, ion channels, phospholipase C, and so forth.

CB-2 Antagonist Development for the Treatment of Psychiatric Disorders

In normal conditions, the expression of CB-2 is low in the brain, but remarkably up-regulated in pathological conditions, such as neurological and psychiatric disorders. Moreover, CB-2 expression is also demonstrated to be associated with neural inflammation, synaptic function, and drug abuse. Besides, CB-2 has been researched as a potential target for the therapy development of psychiatric disorders.

CB-2 antagonist is a therapeutic molecule binding to CB-2 and prevents the binding of natural cannabinoid ligands, which works by inhibiting the biological activities of CB-2. Several CB-2 antagonists have been reported for the treatment and prevention of immune dysfunctions and psychiatric disorders. However, CB-2 antagonist development is relatively challenging since that the CB-2 expression is much higher in peripheral tissues than that in the CNS, thus the antagonist concentration engaging the CNS CB-2 is sufficient to inhibit the activities of CB-2 in peripheral tissues.

CB-2 Antagonist Development Services at Creative Biolabs

Compared with CB-1 antagonist, CB-2 antagonist development for the treatment of psychiatric disorders and other neurological diseases is more challenging. Creative Biolabs is a recognized expert in new drug discovery. We have set up a special scientist team to provide fast and professional novel drug development services for psychiatric disorder treatment. Based on the advanced technology platform, our staff offers global customers fully tailored solutions and services.

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