200 W.-S.V. Ho and C.J. Hillard
Table 4.Inhibitors of AEA cellular uptakeInhibitorCellIC
50(μM)Reference(s)RemarksAM404Primary neurons4–5Beltramo et al. 1997bInhibits FAAH, VR1 agonistVDM 11RBL-2H3 and C6 glioma10–11De Petrocellis et al. 2000Inhibits FAAH, little effect on VR1PC-3 cells11Ruiz-Llorente et al. 2004UCM-707U937 cells0.8Lopez-Rodriguez et al. 2001Moderate inhibition of FAAH, little effect on VR1,binds CBreceptors 2RBL-2H325Fowler et al. 2004C6 glioma41 (max. 50% inhibition)Fowler et al. 2004PC-3 cells25% inhibition at 100 μMRuiz-Llorente et al. 2004UMC-119PC-3 cells11Ruiz-Llorente et al. 2004OMDM-1RBL-2H32.4Ortar et al. 2003; Fowler et al. 2004Ki
:CB—12 μM; FAAH 1>
50 μM; VR1>10 μMC6 glioma>
20Fowler et al. 2004OMDM-2RBL-2H33Ortar et al. 2003Ki: CB—5 μM; FAAH 1>
50 μM; VR1—10 μMRBL-2H33Fowler et al. 2004C6 glioma17 (max. 50% inhibition)Fowler et al. 2004AM1172Cortical neurons2Fegley et al. 2004No inhibition of FAAH at 10 μM;moderate affinity for CBand CB 1;noeffectatVR1 2Please refer to text for the chemical names of the inhibitors.