Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase
…, S Ortega-Gutiérrez, CJ Fowler, G Tiger…
文献索引：Lopez-Rodriguez, Maria L.; Viso, Alma; Ortega-Gutierrez, Silvia; Fowler, Christopher J.; Tiger, Gunnar; De Lago, Eva; Fernandez-Ruiz, Javier; Ramos, Jose A. Journal of Medicinal Chemistry, 2003 , vol. 46, # 8 p. 1512 - 1522 Title/Abstract Full Text View citing articles Show Details Lopez-Rodriguez, Maria L.; Viso, Alma; Ortega-Gutierrez, Silvia; Fowler, Christopher J.; Tiger, Gunnar; De Lago, Eva; Fernandez-Ruiz, Javier; Ramos, Jose A. European Journal of Medicinal Chemistry, 2003 , vol. 38, # 4 p. 403 - 412
A new series of arachidonic acid derivatives were synthesized and evaluated as inhibitors of the endocannabinoid uptake. Most of them are able to inhibit anandamide uptake with IC50 values in the low micromolar range (IC50= 0.8-24 μM). In general, the compounds had only weak effects upon CB1, CB2, and VR1 receptors (K i> 1000-10000 nM). In addition, there was no obvious relationship between the abilities of the compounds to affect anandamide ...
