874902-19-9 Usage
Description
LY-2183240 (874902-19-9) is highly potent inhibitor of cellular anandamide uptake (IC50 = 0.27nM1, 15nM2). LY-2183240 has also been found2-4 to be an inhibitor of fatty acid amide hydrolase (FAAH) – IC50 = 14nM4, diacylglycerol lipase (DAGL) and monoacylglycerol lipase (MAGL) – IC50 = 5.3 nM3.
Uses
LY2183240 is a potent inhibitor of FAAH activity, and the uptake and enzymatic hydrolysis of anandamide. Synthetic Cannabinoids
Biological Activity
Novel and highly potent blocker of anandamide uptake (IC 50 = 270 pM). Inhibits fatty acid amide hydrolase (FAAH) activity (IC 50 = 12.4 nM). Following i.p. administration in rats, increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain.
References
1) Moore et al., (2005), Identification of a high-affinity binding site involved in the transport of endocannabinoids; Proc. Natl. Acad. Sci. USA, 102 17852
2) Ortar et al. (2008), Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revision; Eur. .J. Med. Chem., 43 62
3) Alexander and Cravatt (2006), The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases; J. Am. Chem. Soc., 128 9699
4) Dickason-Chesterfield et al. (2006), Pharmacological Characterization of Endocannabinoid Transport and Fatty Acid Amide Hydrolase Inhibitors; Cell. Mol. Neurobiol., 26 405
Check Digit Verification of cas no
The CAS Registry Mumber 874902-19-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,7,4,9,0 and 2 respectively; the second part has 2 digits, 1 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 874902-19:
(8*8)+(7*7)+(6*4)+(5*9)+(4*0)+(3*2)+(2*1)+(1*9)=199
199 % 10 = 9
So 874902-19-9 is a valid CAS Registry Number.
InChI:InChI=1/C17H17N5O/c1-21(2)17(23)22-16(18-19-20-22)12-13-8-10-15(11-9-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3
874902-19-9Relevant articles and documents
The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases
Alexander, Jessica P.,Cravatt, Benjamin F.
, p. 9699 - 9704 (2006)
How lipid transmitters move within and between cells to communicate signals remains an important and largely unanswered question. Integral membrane transporters, soluble lipid-binding proteins, and metabolic enzymes have all been proposed to collaborative
INHIBITORS OF FATTY ACID AMIDE HYDROLASE AND MONOACYLGLYCEROL LIPASE FOR MODULATION OF CANNABINOID RECEPTORS
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Page/Page column 73, (2009/10/22)
Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.