Chapter category: Neuropharmacology
Cannabinoid Receptors and Signal Transduction
Cannabinoids
Edited by: Vincenzo Di MarzoISBN: 0-306-48228-2
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Chapter authors:
Allyn C. Howlett and Joong-Youn Shim
The cannabinoid receptors are members of the rhodopsin-like family of 7-transmem- brane spanning receptors that are believed to bind their agonist ligands within the central core formed by the interaction of the seven transmembrane helices. Cannabinoid receptors are associated with G proteins of the Gi/o family (Gi 1,2 and 3, and Go1 and 2) via the intracellular loops of the protein. Two receptor subtypes have been characterized: CB1 receptors found predominantly in the nervous system and neuronal cells, and CB2 receptors found predominantly in immune tissue. An alternative receptor that is stimulated by anandamide has been pharmacologically described, and it is coupled to the Gi family of signal transduction proteins. Both CB1 and CB2 cannabinoid receptors inhibit adenylyl cyclase via Gi, and both subtypes stimulate p42/p44 mitogen-activated protein kinase (MAPK) activity. Only the CB1 receptor has been shown to signal via ion channels. CB1 and CB2 receptors influence other signal transduction pathways as well. The molecular mechanism for agonist activation of the cannabinoid receptors involves modification of the conformation of the third and fourth intracellular loops of the receptor such that associated G proteins can be activated.
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