KT109

Description: KT109 is a selective inhibitor of DAGLbeta (IC50 = 42 nM). KT109-treated wild-type mice displayed reductions in LPS-induced allodyni as well as in DAGL-beta (-/-) micea. Repeated KT109 administration prevented the expression of LPS-induced allodynia, without evidence of tolerance. Intraplantar injection of KT109 into the LPS-treated paw, but not the contralateral paw, reversed the allodynic responses. KT109 also reversed allodynia in the CCI and CINP models and lacked discernible side effects (e.g. anxiogenic behaviour, gross motor deficits or gastric ulcers). Target: Others. Smiles: O=C(N1CCCCC1Cc1ccccc1)n1cc(nn1)-c1ccc(cc1)-c1ccccc1. References: Wilkerson JL, Ghosh S, Bagdas D, Mason BL, Crowe MS, Hsu KL, Wise LE, Kinsey SG, Damaj MI, Cravatt BF, Lichtman AH. Diacylglycerol lipase beta inhibition reverses nociceptive behaviour in mouse models of inflammatory and neuropathic pain. Br J Pharmacol. 2016 May,173(10):1678-92. doi: 10.1111/bph.13469. PubMed PMID: 26915789, PubMed Central PMCID: PMC4842918.