| Name | Fatty acid amide hydrolase |
|---|---|
| Synonyms | Anandamide amidohydrolase; FAAH; Fatty acid amide hydrolase; Oleamide hydrolase; Oleamide hydrolase Anandamide amidohydrolase FAAH; Fatty acid amide hydrolases; Oleamide hydrolases; Oleamide hydrolase Anandamide amidohydrolase FAAHs |
| Name | biphenyl |
|---|---|
| CAS | 1,1′-biphenyl |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 19290863 | Lodola A, Mor M, Sirirak J, Mulholland AJ: Insights into the mechanism and inhibition of fatty acid amide hydrolase from quantum mechanics/molecular mechanics (QM/MM) modelling. Biochem Soc Trans. 2009 Apr;37(Pt 2):363-7. |
2(0,0,0,2) | Details |
| 19583260 | Matuszak N, Muccioli GG, Labar G, Lambert DM: Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors. J Med Chem. 2009 Dec 10;52(23):7410-20. Biol. 2005 , 12 , 649 - 656 ) as MGL inhibitors, and along these lines, we present a new set of maleimide derivatives that showed low micromolar IC (50) and high selectivity toward MGL vs FAAH. Then, structure-activity relationships have been investigated and, for instance, 1-biphenyl-4-ylmethylmaleimide inhibits MGL with an IC (50) value of 790 nM. |
1(0,0,0,1) | Details |
| 17944864 | Vinod KY, Sanguino E, Yalamanchili R, Manzanares J, Hungund BL: Manipulation of fatty acid amide hydrolase functional activity alters sensitivity and dependence to J Neurochem. 2008 Jan;104(1):233-43. Epub 2007 Oct 17. The deletion of FAAH gene or the inhibition of FAAH by carbamoyl-biphenyl-3-yl-cyclohexylcarbamate (URB597) (0.1 mg/kg) markedly increased the preference for |
88(1,1,1,8) | Details |
| 18762181 | Haller VL, Stevens DL, Welch SP: Modulation of opioids via protection of degradation by fatty acid amide hydrolase. Eur J Pharmacol. 2008 Dec 14;600(1-3):50-8. Epub 2008 Aug 20. Cyclohexylcarbamic acid 3'-carbamoyl-biphenyl-3-yl ester (URB597) is an inhibitor of FAAH, increases brain levels and enhances -induced antinociception in male ICR mice (25-30 g). |
83(1,1,1,3) | Details |
| 18507372 | Mor M, Lodola A, Rivara S, Vacondio F, Duranti A, Tontini A, Sanchini S, Piersanti G, Clapper JR, King AR, Tarzia G, Piomelli D: Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates. J Med Chem. 2008 Jun 26;51(12):3487-98. Epub 2008 May 29. |
68(0,2,3,3) | Details |
| 19826190 | Adamczyk P, McCreary AC, Przegalinski E, Mierzejewski P, Bienkowski P, Filip M: The effects of fatty acid amide hydrolase inhibitors on maintenance of cocaine and food self-administration and on reinstatement of cocaine-seeking and food-taking behavior in rats. J Physiol Pharmacol. 2009 Sep;60(3):119-25. The present study aimed to examine the effect of the FAAH inhibitors, phenylmethylsulphonyl (PMSF; i.p.) or cyclohexylcarbamic acid 3-carbamoyl biphenyl-3-yl ester (URB597; i.p.) on the cocaine- or food-maintained self-administration as well as on the cocaine-seeking or food-taking behaviors in rats. |
34(0,1,1,4) | Details |
| 18724387 | Sagar DR, Kendall DA, Chapman V: Inhibition of fatty acid amide hydrolase produces PPAR-alpha-mediated analgesia in a rat model of inflammatory pain. Br J Pharmacol. 2008 Dec;155(8):1297-306. Epub 2008 Aug 25. Here, the effects of the FAAH inhibitor URB597 (3'-carbamoyl-biphenyl-3-yl-cyclohexylcarbamate) on responses of spinal neurons were studied. |
33(0,1,1,3) | Details |
| 19197005 | Antonelli T, Tomasini MC, Mazza R, Fuxe K, Gaetani S, Cuomo V, Tanganelli S, Ferraro L: Cannabinoid CB1 and cholecystokinin CCK2 receptors modulate, in an opposing way, electrically evoked [3H] efflux from rat cerebral cortex cell cultures: possible relevance for cortical transmission and anxiety. J Pharmacol Exp Ther. 2009 May;329(2):708-17. Epub 2009 Feb 5. The effects of treatments with cannabinoid (CB)(1) and cholecystokinin (CCK)(2) receptor agonists and antagonists, as well as compounds that enhance endocannabinoid signaling by inhibiting degradation, e.g., the fatty acid amide hydrolase inhibitor 3'-carbamoyl-biphenyl-3-yl-cyclohexylcarbamate (URB597) or the endocannabinoid reuptake inhibitor (5Z,8Z,11Z,14Z)-N-(3-furanylmethyl)-5,8,11,14-eicosatetraenamide (UCM707), were studied both on spontaneous and electrically evoked [(3) H] efflux from rat cerebral cortex cell cultures. |
31(0,1,1,1) | Details |
| 19118134 | Naidu PS, Booker L, Cravatt BF, Lichtman AH: Synergy between enzyme inhibitors of fatty acid amide hydrolase and cyclooxygenase in visceral nociception. J Pharmacol Exp Ther. 2009 Apr;329(1):48-56. Epub 2008 Dec 31. The cannabinoid receptor 1 (CB (1)) receptor antagonist, rimonabant, but not the cannabinoid receptor 2 (CB (2)) receptor antagonist, SR144528, blocked the antinociceptive phenotype of FAAH (-/-) mice and the analgesic effects of URB597 (3'-carbamoyl-biphenyl-3-yl-cyclohexylcarbamate) or OL-135 (1-oxo-1 [5-(2-pyridyl)-2-yl]-7-phenyl heptane), respective irreversible and reversible FAAH inhibitors, administered to C57BL/6 mice. |
6(0,0,0,6) | Details |
| 18416822 | Richardson D, Pearson RG, Kurian N, Latif ML, Garle MJ, Barrett DA, Kendall DA, Scammell BE, Reeve AJ, Chapman V: Characterisation of the cannabinoid receptor system in synovial tissue and fluid in patients with osteoarthritis and rheumatoid arthritis. Arthritis Res Ther. 2008;10(2):R43. Epub 2008 Apr 16. FAAH was active in the synovia of OA and RA patients and was sensitive to inhibition by URB597 (3'-(aminocarbonyl) [1,1'-biphenyl]-3-yl)-cyclohexylcarbamate). |
32(0,1,1,2) | Details |
| 17868306 | Degn M, Lambertsen KL, Petersen G, Meldgaard M, Artmann A, Clausen BH, Hansen SH, Finsen B, Hansen HS, Lund TM: Changes in brain levels of N-acylethanolamines and 2-arachidonoylglycerol in focal cerebral ischemia in mice. J Neurochem. 2007 Dec;103(5):1907-16. Epub 2007 Sep 14. Treatment with the fatty acid amide hydrolase inhibitor URB597 (cyclohexyl 3'-carbamoyl-biphenyl-3-yl ester; 1 mg/kg; i.p.) 1.5 h before arterial occlusion decreased the infarct volume in our model system. |
31(0,1,1,1) | Details |
| 18675915 | Fowler CJ, Ghafouri N: Does the hydrolysis of 2-arachidonoylglycerol regulate its cellular uptake?. Pharmacol Res. 2008 Jul;58(1):72-6. Epub 2008 Jul 15. The selective fatty acid amide hydrolase inhibitor URB597 (3'-(aminocarbamoyl)[1,1'-biphenyl]-3-yl)-cyclohexylcarbamate) completely blocked the hydrolysis of and reduced its uptake by about half in RBL2H3 basophilic leukaemia cells. |
31(0,1,1,1) | Details |
| 19637155 | Clapper JR, Vacondio F, King AR, Duranti A, Tontini A, Silva C, Sanchini S, Tarzia G, Mor M, Piomelli D: A second generation of -based fatty acid amide hydrolase inhibitors with improved activity in vivo. ChemMedChem. 2009 Sep;4(9):1505-13. |
6(0,0,0,6) | Details |
| 18027904 | Ortar G, Cascio MG, De Petrocellis L, Morera E, Rossi F, Schiano-Moriello A, Nalli M, de Novellis V, Woodward DF, Maione S, Di Marzo V: New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. J Med Chem. 2007 Dec 27;50(26):6554-69. Epub 2007 Nov 21. N-arachidonoylserotonin (AA-5-HT, 1a) is an inhibitor of fatty acid amide hydrolase (FAAH) that acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels and is analgesic in rodents. |
4(0,0,0,4) | Details |
| 18247553 | Kimball FS, Romero FA, Ezzili C, Garfunkle J, Rayl TJ, Hochstatter DG, Hwang I, Boger DL: Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. J Med Chem. 2008 Feb 28;51(4):937-47. Epub 2008 Feb 5. |
4(0,0,0,4) | Details |
| 19702785 | Gardiner SM, March JE, Kemp PA, Bennett T: Factors influencing the regional haemodynamic responses to methanandamide and in conscious rats. Br J Pharmacol. 2009 Oct;158(4):1143-52. Epub 2009 Aug 20. BACKGROUND AND PURPOSE: In vitro evidence suggests that metabolism of by cyclooxygenase-2 (COX-2) may be more important when the primary metabolic pathway [i.e. fatty acid amide hydrolase (FAAH)] is inhibited. KEY RESULTS: Inhibition of FAAH with URB597 (cyclohexycarbamic acid 3'-carbamoyl-biphenyl-3-yl-ester) augmented the haemodynamic actions of but there was no effect of COX-2 inhibition with parecoxib, either in the absence or the presence of URB597. |
2(0,0,0,2) | Details |