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Discovery and development of endocannabinoid-hydrolyzing enzyme inhibitors.
Curr Top Med Chem 2010; 10(8):828-58CT

Abstract

Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are hydrolytic enzymes which degrade the endogenous cannabinoids (endocannabinoids) N-arachidonoylethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG), respectively. Endocannabinoids are an important class of lipid messenger molecules that are produced on demand in response to elevated intracellular calcium levels. They recognize and activate the cannabinoid CB(1) and CB(2) receptors, the molecular targets for Delta(9)-tetrahydrocannabinol (Delta(9)-THC) in marijuana evoking several beneficial therapeutic effects. However, in vivo the cannabimimetic effects of AEA and 2-AG remain weak owing to their rapid inactivation by FAAH and MGL, respectively. The inactivation of FAAH and MGL by specific enzyme inhibitors increases the levels of AEA and 2-AG, respectively, producing therapeutic effects such as pain relief and depression of anxiety.

Authors+Show Affiliations

School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio, Finland. anna.minkkila@uef.fiNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

20370710

Citation

Minkkilä, Anna, et al. "Discovery and Development of Endocannabinoid-hydrolyzing Enzyme Inhibitors." Current Topics in Medicinal Chemistry, vol. 10, no. 8, 2010, pp. 828-58.
Minkkilä A, Saario S, Nevalainen T. Discovery and development of endocannabinoid-hydrolyzing enzyme inhibitors. Curr Top Med Chem. 2010;10(8):828-58.
Minkkilä, A., Saario, S., & Nevalainen, T. (2010). Discovery and development of endocannabinoid-hydrolyzing enzyme inhibitors. Current Topics in Medicinal Chemistry, 10(8), pp. 828-58.
Minkkilä A, Saario S, Nevalainen T. Discovery and Development of Endocannabinoid-hydrolyzing Enzyme Inhibitors. Curr Top Med Chem. 2010;10(8):828-58. PubMed PMID: 20370710.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Discovery and development of endocannabinoid-hydrolyzing enzyme inhibitors. AU - Minkkilä,Anna, AU - Saario,Susanna, AU - Nevalainen,Tapio, PY - 2009/09/23/received PY - 2010/01/27/accepted PY - 2010/4/8/entrez PY - 2010/4/8/pubmed PY - 2011/5/3/medline SP - 828 EP - 58 JF - Current topics in medicinal chemistry JO - Curr Top Med Chem VL - 10 IS - 8 N2 - Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are hydrolytic enzymes which degrade the endogenous cannabinoids (endocannabinoids) N-arachidonoylethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG), respectively. Endocannabinoids are an important class of lipid messenger molecules that are produced on demand in response to elevated intracellular calcium levels. They recognize and activate the cannabinoid CB(1) and CB(2) receptors, the molecular targets for Delta(9)-tetrahydrocannabinol (Delta(9)-THC) in marijuana evoking several beneficial therapeutic effects. However, in vivo the cannabimimetic effects of AEA and 2-AG remain weak owing to their rapid inactivation by FAAH and MGL, respectively. The inactivation of FAAH and MGL by specific enzyme inhibitors increases the levels of AEA and 2-AG, respectively, producing therapeutic effects such as pain relief and depression of anxiety. SN - 1873-4294 UR - https://www.unboundmedicine.com/medline/citation/20370710/Discovery_and_development_of_endocannabinoid_hydrolyzing_enzyme_inhibitors_ L2 - http://www.eurekaselect.com/85469/article DB - PRIME DP - Unbound Medicine ER -