| Identification | Back Directory | [Name]
5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE | [CAS]
874902-19-9 | [Synonyms]
CS-752
LY 2183240
LY2183240 powder
LY-2183240 MN-25
LY2183240/LY-2183240
N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide
5-(biphenyl-4-ylMethyl)-N,N-diMethyl-1H-tetrazole-1-carboxaMide
5-Biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide
5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE
1H-Tetrazole-1-carboxamide, 5-([1,1′-biphenyl]-4-ylmethyl)-N,N-dimethyl- | [Molecular Formula]
C17H17N5O | [MDL Number]
MFCD08703123 | [MOL File]
874902-19-9.mol | [Molecular Weight]
307.35 |
| Chemical Properties | Back Directory | [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). | [form ]
White to off-white solid. | [pka]
0.01±0.10(Predicted) | [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 |
| Hazard Information | Back Directory | [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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