title: Constitutive activity in cannabinoid receptors.
abstract: The cannabinoid receptors are G protein-coupled receptors activated by endocannabinoids or exogenous agonist such as tetrahydrocannabinol. Upon agonist binding, cannabinoid receptors will activate G proteins of the Gi family, which in turn inhibits adenylyl cyclase. Recently, inverse agonists and neutral antagonist for cannabinoid receptors have been discovered, demonstrating constitutive activity of the cannabinoid receptors. This chapter will discuss the current state of the art and provide a framework for evaluating constitutive receptor activity and distinguishing constitutive receptor activity from constitutive endogenous agonist tone.
authors.affiliation: Forest Research Institute, Jersey City, New Jersey, USA. Electronic address: tungfong123@yahoo.com.
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
mesh_terms: D000818:Animals; D001681:Biological Assay; D000242:Cyclic AMP / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D009154:Mutation / Q000235:genetics*; D043882:Receptors, Cannabinoid / Q000235:genetics* / Q000378:metabolism*; D013816:Thermodynamics
chemical_list: D043882:Receptors, Cannabinoid; D000242:Cyclic AMP
keywords: cannabinoid receptor; endocannabinoid; forskolin; inverse agonist; neutral antagonist; slice electrophysiology