5-[[(1,1'-Biphenyl)-4-yl]methyl]-N,N-dimethyl-1H-tetrazole-1-carboxamide

Product Name5-[[(1,1'-Biphenyl)-4-yl]methyl]-N,N-dimethyl-1H-tetrazole-1-carboxamide
CAS874902-19-9
MFC17H17N5O
MW307.35
EINECS
MOL File874902-19-9.mol

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

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.

in vivo

LY2183240 (3-30mg/kg; i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms^[1].

Animal Model:	Male Sprague-Dawley rats (Formalin Pain Model)^[1]
Dosage:	3, 10, 30 mg/kg
Administration:	I.p.
Result:	Dose-dependently attenuated formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms.

References

[1] S A MOORE. Identification of a high-affinity binding site involved in the transport of endocannabinoids.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 49: 17852-17857. DOI:10.1073/pnas.0507470102
[2] GIORGIO ORTAR . Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revisitation[J]. European Journal of Medicinal Chemistry, 2008, 43 1: Pages 62-72. DOI:10.1016/j.ejmech.2007.02.023
[3] JESSICA P. ALEXANDER Benjamin F C. The Putative Endocannabinoid Transport Blocker LY2183240 Is a Potent Inhibitor of FAAH and Several Other Brain Serine Hydrolases[J]. Journal of the American Chemical Society, 2006, 128 30: 9699-9704. DOI:10.1021/ja062999h
[4] AMY K DICKASON-CHESTERFIELD. Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors.[J]. Cellular and Molecular Neurobiology, 2006, 26 4-6: 407-423. DOI:10.1007/s10571-006-9072-6

5-[[(1,1'-Biphenyl)-4-yl]methyl]-N,N-dimethyl-1H-tetrazole-1-carboxamide Supplier

5-[[(1,1'-Biphenyl)-4-yl]methyl]-N,N-dimethyl-1H-tetrazole-1-carboxamide manufacturers

Related Product Information

Send Inquriy