Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo

Proceedings of the National Academy of Sciences of the United States of America

Volumn 106, Issue 48, 2009, Pages 20270-20275

  Long, Jonathan Z ^a   Nomura, Daniel K ^a   Vann, Robert E ^b   Walentiny, D Matthew ^b   Booker, Lamont ^b   Jin, Xin ^a   Burston, James J ^b   Sim Selley, Laura J ^b   Lichtman, Aron H ^b   Wiley, Jenny L ^b   Cravatt, Benjamin F ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

^b VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

Author keywords

Hydrolase; Inhibitor; Metabolism

Indexed keywords

2 ARACHIDONOYLGLYCEROL; ACYLGLYCEROL LIPASE; ACYLGLYCEROL LIPASE INHIBITOR; ANANDAMIDE; CANNABINOID 1 RECEPTOR; CANNABINOID RECEPTOR ANTAGONIST; DRONABINOL; ENDOCANNABINOID; ENZYME INHIBITOR; FATTY ACID AMIDASE; FATTY ACID AMIDASE INHIBITOR; JZL 184; JZL 195; PF 3845; RIMONABANT; UNCLASSIFIED DRUG;

ANALGESIA; ANALGESIC ACTIVITY; ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ANTINOCICEPTION; ARTICLE; CATALEPSY; CONTROLLED STUDY; DRUG ABUSE; DRUG DISCRIMINATION; ENZYME INHIBITION; HYPOTHERMIA; IN VIVO STUDY; MOTOR DYSFUNCTION; MOUSE; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION;

AMIDOHYDROLASES; ANIMALS; ARACHIDONIC ACIDS; CARBAMATES; CARBOXYLIC ESTER HYDROLASES; ENDOCANNABINOIDS; GLYCERIDES; MICE; MOLECULAR STRUCTURE; MONOACYLGLYCEROL LIPASES; MOTOR ACTIVITY; PAIN MEASUREMENT; PIPERIDINES; POLYUNSATURATED ALKAMIDES;

CANNABIS SATIVA; MAMMALIA;

EID: 73949109254     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.0909411106     Document Type: Article

References (46)

1. Devane WA, et al. (1992) Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 258:1946-1949.
2. Mechoulam R, et al. (1995) Identification of an endogenous 2-monoglyceride, present in canine gut, that binds cannabinoid receptors. Biochem Pharmacol 50:83-90.
3. Sugiura T, et al. (1995) 2-Arachidonylglycerol: A possible endogenous cannabinoid receptor ligand in brain. Biochem Biophys Res Commun 215:89-97.
4. Di Marzo V, Bisogno T, De Petrocellis L (2007) Endocannabinoids and related compounds: Walking back and forth between plant natural products and animal physiology. Chem Biol 14:741-756.
5. Zimmer A, Zimmer AM, Hohmann AG, Herkenham M, Bonner TI (1999) Increased mortality, hypoactivity, and hypoalgesia in cannabinoid CB1 receptor knockout mice. Proc Natl Acad Sci 96:5780-5785.
6. Ledent C, et al. (1999) Unresponsiveness to cannabinoids and reduced addictive effects of opiates in CB1 receptor knockout mice. Science 283:401-404.
7. Freund TF, Katona I, Piomelli D (2003) Role of endogenous cannabinoids in synaptic signaling. Physiol Rev 83:1017-1066.
8. Egertova M, Giang DK, Cravatt BF, Elphick MR (1998) A new perspective on cannabinoid signalling: Complimentary localization of fatty acid amide hydrolase and the CB1 receptor in rat brain. Proc R Soc Lond B 265:2081-2085.
9. Cravatt BF, Lichtman AH (2003) Fatty acid amide hydrolase: An emerging therapeutic target in the endocannabinoid system. Curr Opin Chem Biol 7:469-475.
10. Piomelli D (2005) The endocannabinoid system: A drug discovery perspective. Curr Opin Investig Drugs 6:672-679.
11. Jonsson KO, Holt S, Fowler CJ (2006) The endocannabinoid system: Current pharmacological research and therapeutic opportunities. Basic Clin Pharmacol Toxicol 98:124-134.
12. Koutek B, et al. (1994) Inhibitors of arachidonyl ethanolamide hydrolysis. J Biol Chem 269:22937-22940.
13. Ahn K, McKinney MK, Cravatt BF (2008) Enzymatic pathways that regulate endocannabinoid signaling in the nervous system. Chem Rev 108:1687-1707.
14. Cravatt BF, et al. (1996) Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides. Nature 384:83-87.
15. Deutsch DG, Ueda N, Yamamoto S (2002) The fatty acid amide hydrolase (FAAH). Prostaglandins Leuko Essent Fatty Acids 66:201-210.
16. McKinney MK, Cravatt BF (2005) Structure and function of Fatty acid amide hydrolase. Annu Rev Biochem 74:411-432.
17. Blankman JL, Simon GM, Cravatt BF (2007) A comprehensive profile of brain enzymes that hydrolyze the endocannabinoid 2-arachidonoylglycerol.ChemBiol 14:1347-1356.
18. Cravatt BF, et al. (2001) Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice lacking fatty acid amide hydrolase. Proc Natl Acad Sci USA 98:9371-9376.
19. Ahn K, et al. (2009) Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem Biol 16:411-420.
20. Kathuria S, et al. (2003) Modulation of anxiety through blockade of anandamide hydrolysis. Nat Med 9:76-81.
21. Saghatelian A, et al. (2004) Assignment of endogenous substrates to enzymes by global metabolite profiling. Biochemistry 43:14332-14339.
22. Osei-Hyiaman D, et al. (2005) Cocaine- and amphetamine-related transcript is involved in the orexigenic effect of endogenous anandamide. Neuroendocrinology 81:273-282.
23. Long JZ, et al. (2009) Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects. Nat Chem Biol 5:37-44.
24. Long JZ, Nomura DK, Cravatt BF (2009) Characterization of monoacylglycerol lipase inhibition reveals differences in central and peripheral endocannabinoid metabolism. Chem Biol 16:744-753.
25. Russo R, et al. (2007) The fatty acid amide hydrolase inhibitor URB597 (cyclohexylcarbamic acid 3′-carbamoylbiphenyl-3-yl ester) reduces neuropathic pain after oral administration in mice. J Pharmacol Exp Ther 322:236-242.
26. Lichtman AH, et al. (2004) Reversible inhibitors of fatty acid amide hydrolase that promote analgesia: Evidence for an unprecedented combination of potency and selectivity. J Pharmacol Exp Ther 311:441-448.
27. Kinsey SG, et al. (2009) Blockade of endocannabinoid-degrading enzymes attenuates neuropathic pain. J Pharmacol Exp Ther.
28. Solinas M, et al. (2007) The endogenous cannabinoid anandamide produces delta-9-tetrahydrocannabinol-like discriminative and neurochemical effects that are enhanced by inhibition of fatty acid amide hydrolase but not by inhibition of anandamide transport. J Pharmacol Exp Ther 321:370-380.
29. Nomura DK, et al. (2008) Activation of the endocannabinoid system by organophosphorus nerve agents. Nat Chem Biol 4:373-378.
30. Nomura DK, et al. (2008) Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels. Bioorg Med Chem Lett 18:5875-5878.
31. AhnK, et al. (2007) Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. Biochemistry 46:13019-13030.
32. Patricelli MP, Giang DK, Stamp LM, Burbaum JJ (2001) Direct visualization of serine hydrolase activities in complex proteome using fluorescent active site-directed probes. Proteomics 1:1067-1071.
33. Leung D, Hardouin C, Boger DL, Cravatt BF (2003) Discovering potent and selective inhibitors of enzymes in complex proteomes. Nat Biotechnol 21:687-691.
34. Winrow CJ, et al. (2003) Loss of neuropathy target esterase in mice links organophosphate exposure to hyperactivity. Nat Genet 33:477-485.
35. Johnson MK, Glynn P (1995) Neuropathy target esterase (NTE) and organophosphorusinduced delayed polyneuropathy (OPIDP): Recent advances. Toxicol Lett 82:459-463.
36. Jessani N, et al. (2005) A streamlined platform for high-content functional proteomics of primary human specimens. Nat Methods 2:691-697.
37. Fegley D, et al. (2005) Characterization of the fatty acid amide hydrolase inhibitor cyclohexyl carbamic acid 3′-carbamoyl-biphenyl-3-yl ester (URB597): Effects on anandamide and oleoylethanolamide deactivation. J Pharmacol Exp Ther 313:352-358.
38. Smith PB, et al. (1994) The pharmacological activity of anandamide, a putative endogenous cannabinoid, in mice. J Pharmacol Exp Ther 270:219-227.
39. Patel S, Hillard CJ (2001) Cannabinoid CB(1) receptor agonists produce cerebellar dysfunction in mice. J Pharmacol Exp Ther 297:629-637.
40. Balster RL, Prescott WR (1992) Delta 9-tetrahydrocannabinol discrimination in rats as a model for cannabis intoxication. Neurosci Biobehav Rev 16:55-62.
41. Gobbi G, et al. (2005) Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis. Proc Natl Acad Sci USA 102:18620-18625.
42. Siegel GJ, Agranoff BW, Albers RW, Molinoff PB (1994) Basic Neurochemistry (Raven Press, New York).
43. Solinas M, Panlilio LV, Justinova Z, Yasar S, Goldberg SR (2006) Using drug-discrimination techniques to study the abuse-related effects of psychoactive drugs in rats. Nat Protoc 1:1194-1206.
44. Schlosburg JE, et al. (2009) Inhibitors of endocannabinoid-metabolizing enzymes reduce precipitated withdrawal responses in THC-dependent mice. AAPS J 11:342-352.
45. Melis M, et al. (2008) Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors. J Neurosci 28:13985-13994.
46. Merritt LL, Martin BR, Walters C, Lichtman AH, Damaj MI (2008) The endogenous cannabinoid system modulates nicotine reward and dependence. J Pharmacol Exp Ther 326:483-492.