5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE Chemical Properties

Melting point:

87-88℃

Boiling point:

506.1±53.0 °C(Predicted)

Density 

1.21

storage temp. 

Sealed in dry,2-8°C

solubility 

Soluble in DMSO (greater than 25 mg/ml) or in Ethanol (up to 15 mg/ml).

pka

0.01±0.10(Predicted)

form 

White to off-white solid.

color 

White

Stability:

Stable for 1 year as supplied. Solutions in DMSO of ethanol may be stored at -20°C for up to 1 month

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE Usage And Synthesis

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

Definition

ChEBI: N,N-dimethyl-5-[(4-phenylphenyl)methyl]-1-tetrazolecarboxamide is a member of biphenyls.

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

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