OMDM-2は代謝的に安定で、強力な細胞内アナンダミド取り込み阻害剤である(神経細胞(C6グリオーマ細胞):IC50 = 3.2 µM;非神経細胞(ラットRBL-2H3細胞):IC50 = 17 µM)、CB1受容体(CB1: Ki = 5.1 µM、CB2: Ki > 10 µM)、TRPV1(EC50 = 10 µM)およびFAAH(IC50 > 100 µM)に対する作用はごくわずかであった。
OMDM-2 参考文献
Novel selective and metabolically stable inhibitors of anandamide cellular uptake: G. Ortar, et al.; Biochem. Pharmacol. 65, 1473 (2003) Selective inhibition of anandamide cellular uptake versus enzymatic hydrolysis--a difficult issue to handle: C.J. Fowler, et al.; Eur. J. Pharmacol. 492, 1 (2004) Further evidence for the existence of a specific process for the membrane transport of anandamide: A. Ligresti, et al.; Biochem. J. 380, 265 (2004) In vivo pharmacological actions of two novel inhibitors of anandamide cellular uptake: E. de Lago, et al.; Eur. J. Pharmacol. 484, 249 (2004)