Cannabinoids and the Cannabinoid Receptors: An Overview
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2017 Elsevier Inc. All rights reserved. Cannabis is the most popular illicit drug in the Western world, and has a long history of medical use. Its active ingredients, known as cannabinoids, can elicit various biological activities through activation of certain G-protein coupled receptors, denoted by the name of cannabinoid receptors. By far, two cannabinoid receptors have been identified, namely the cannabinoid receptor 1 (CB1) and 2 (CB2). The CB1 receptors are primarily found in the central nervous system (CNS) while the CB2 receptors largely present in the periphery. Besides the plant-derived cannabinoids (phytocannabinoids), a group of endogenous lipid-derived molecules can similarly activate the cannabinoid receptors; therefore they are referred to as endocannabinoids. Activation and blockade of cannabinoid receptors can lead to a variety of responses relevant to pharmacotherapy. This chapter provides a synopsis of phytocannabinoids, and an overview of cannabinoid receptors with respects to: what they are; where they are; and what they do.