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Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists Lunn CA; Reich EP; Fine JS; Lavey B; Kozlowski JA; Hipkin RW; Lundell DJ; Bober LBr J Pharmacol 2008[Jan]; 153 (2): 226-39Evidence has emerged suggesting a role for the cannabinoid CB2 receptor in immune cell motility. This provides a rationale for a novel and generalized immunoregulatory role for cannabinoid CB2 receptor-specific compounds. In support of this possibility, we will review the biology of a class of cannabinoid CB2 receptor-specific inverse agonist, the triaryl bis-sulfones. We will show that one candidate, Sch.414319, is potent and selective for the cannabinoid CB2 receptor, based on profiling studies using biochemical assays for 45 enzymes and 80 G-protein coupled receptors and ion channels. We will describe initial mechanistic studies using this optimized triaryl bis-sulfone, showing that the compound exerts a broad effect on cellular protein phosphorylations in human monocytes. This profile includes the down regulation of a required phosphorylation of the monocyte-specific actin bundling protein L-plastin. We suggest that this observation may provide a mechanism for the observed activity of Sch.414319 in vivo. Our continued analysis of the in vivo efficacy of this compound in diverse disease models shows that Sch.414319 is a potent modulator of immune cell mobility in vivo, can modulate bone damage in antigen-induced mono-articular arthritis in the rat, and is uniquely potent at blocking experimental autoimmune encephalomyelitis in the rat.|Amino Acid Sequence[MESH]|Animals[MESH]|Autoimmune Diseases/drug therapy/physiopathology[MESH]|Cell Movement/drug effects/physiology[MESH]|Humans[MESH]|Immunity, Cellular/drug effects/physiology[MESH]|Molecular Sequence Data[MESH]|Receptor, Cannabinoid, CB2/*agonists/genetics[MESH]|Sulfones/chemistry/pharmacology[MESH] |
