2004
DOI: 10.1124/jpet.104.078980
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Characterization of the Fatty Acid Amide Hydrolase Inhibitor Cyclohexyl Carbamic Acid 3′-Carbamoyl-biphenyl-3-yl Ester (URB597): Effects on Anandamide and Oleoylethanolamide Deactivation

Abstract: Fatty acid amide hydrolase (FAAH) is an intracellular serine enzyme that catalyzes the hydrolysis of bioactive fatty acid ethanolamides such as anandamide and oleoylethanolamide (OEA). Genetic deletion of the faah gene in mice elevates brain anandamide levels and amplifies the effects of this endogenous cannabinoid agonist. Here, we show that systemic administration of the selective FAAH inhibitor URB597 (cyclohexyl carbamic acid 3Ј-carbamoyl-biphenyl-3-yl ester; 0.3 mg/kg i.p.) increases anandamide levels in … Show more

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Cited by 400 publications
(380 citation statements)
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“…These data differ somewhat from observations in rat, and may be related to the much higher affinity of JNJ‐42165279 for human over rat FAAH. 4 Moreover, inactivation of OEA and PEA may be mediated by other mechanisms in addition to FAAH 12, 13, 14. Effects on FAA turnover and leukocyte FAAH activity consistent with this report have been observed previously with PF‐04457845.…”
Section: Discussionsupporting
confidence: 81%
“…These data differ somewhat from observations in rat, and may be related to the much higher affinity of JNJ‐42165279 for human over rat FAAH. 4 Moreover, inactivation of OEA and PEA may be mediated by other mechanisms in addition to FAAH 12, 13, 14. Effects on FAA turnover and leukocyte FAAH activity consistent with this report have been observed previously with PF‐04457845.…”
Section: Discussionsupporting
confidence: 81%
“…URB597 is a potent, selective and systemically active inhibitor of FAAH (Kathuria et al 2003;Fegley et al 2005) that increases endogenous anandamide levels and facilitates endocannabinoid neurotransmission (Kathuria et al 2003). Recently, this compound was shown to exert profound anxiolytic-and antidepressant-like activities in rodents; these activities were prevented by the CB1 receptor antagonist rimonabant and were not accompanied by overt rewarding effects (Kathuria et al 2003;Gobbi et al 2005).…”
Section: Introductionmentioning
confidence: 99%
“…Noteworthy, the effects produced by AM404 are markedly different from those exerted by the FAAH inhibitor URB597 in at least two respects. First, AM404 does not affect brain levels of OEA and PEA, which are enhanced by URB597 (Kathuria et al, 2003;Fegley et al, 2005). Second, although AM404 mirrors the anxiolytic-like effects of URB597 (Kathuria et al, 2003), the latter does not exert any significant motivational effect in the CPP model, irrespective of housing conditions (Gobbi et al, 2005).…”
Section: Discussionmentioning
confidence: 93%