A Brief Introduction to Cannabinoid Receptors
In humans, cannabinoid receptors (CBRs) are a category of cell membrane receptors for the binding of endogenous and exogenous cannabinoids. CBRs are members of the G protein-coupled receptor superfamily that characterized by seven transmembrane spanning domains. As one of the most widely distributed receptors in the body, CBRs also are an important part of the endocannabinoid system, a critical neuromodulatory system responsible for the synaptic plasticity and homeostatic processes in the brain.
Although the usage of the plant Cannabis sativa, also known as marijuana, can be dated back to thousands of years ago in China, the CBRs (firstly cannabinoid receptor type 1) were discovered and identified in the 1980s and cloned in late 1990. Currently, two known subtypes CBRs have been identified, including cannabinoid receptor type 1 (CB1R) and cannabinoid receptor type 2 (CB2R), and other additional CBRs are being or to be discovered.
Cannabinoid Receptor Signaling and Psychiatric Disorders
CBRs can be activated by endocannabinoids, such as arachidonylethanolamine and 2-arachidonylglycerol, also bind to exocannabinoids, including both plant cannabinoids (e.g., tetrahydrocannabinol) and synthetic cannabinoids. Once the CBRs are engaged, multiple and complicate intracellular signal transduction pathways will be activated. Evidence indicated that the activation of CBRs firstly inhibited the activity of adenylyl cyclase, and then had an influence on the activities of ion channels, protein kinases, JNK, p38, and many other related pathways. All these pathways and activities enable CBRs to be involved in many physiological and biological processes.
CBRs are one of the most abundant receptors in the central nervous system (CNS), which are largely involved in various central neural activities and disorders, widely including appetite, pain-sensation, mood, memory, schizophrenia, multiple sclerosis, neurodegeneration, and psychiatric disorders. And increasing investigations demonstrated that CBRs and related ligands are promising targets for the treatment development of psychiatric disorders.
Cannabinoid Receptor Regulators
Considering the importance of the cannabinoid receptor, mounting attention has been paid to the cannabinoid receptor as novel therapeutic targets for the development of novel therapies for neurological disorders. Cannabinoid receptor regulators are a class of molecules designed to attenuate or enhance endocannabinoid transmission and inhibit or increase the activity of the CBRs to gain therapeutic effects on some psychiatric diseases, such as anxiety disorders and mood disorders. At present, cannabinoid receptor regulator exploration is not limited to the receptors, but also focuses on the possible ligands and interacting molecules. By blocking or enhancing the interaction between these ligands with the receptors will also regulate the CBR-mediated pathways and their activities.
Services
Since the first description of the CBRs, the research and development of molecular drugs targeting the cannabinoid receptor have never stopped. Despite impressive advances that have been made in pharmacological therapies for the treatment of psychiatric diseases, there is still much room for improvement in the exploration of cannabinoid receptor regulators for psychiatric disorder treatment.
As a pioneer and the undisputed global leader in novel drug discovery and manufacturing, Creative Biolabs has won a good reputation in providing high-quality services and support for the development of cannabinoid receptor regulators. Based on powerful solid technologies and years of experience, our professional scientists are glad to provide a range of tailored strategies and services for the development of cannabinoid receptor regulators, which mainly include but not limited to:
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