LY 2183240

Cat. No. 2452

LY 2183240 C17H17N5O [874902-19-9]

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

Biological Activity

Novel and highly potent blocker of anandamide uptake (IC50 = 270 pM). Inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). Following i.p. administration in rats, increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain.

Licensing Information

Sold under license from Eli Lilly and Company

Technical Data

M.Wt:
307.35
Formula:
C17H17N5O
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol with gentle warming
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
874902-19-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Alexander and Cravat (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. PMID: 16866524.

Dickason-Chesterfield et al (2006) Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol.Neurobiol. 26 407. PMID: 16736384.

Moore et al (2005) Identification of a high-affinity binding site involved in the transport of endocannabinoids. Proc.Natl.Acad.Sci.USA 102 17852.

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Citations are publications that use Tocris products. Selected citations for LY 2183240 include:

Gonzalez-Islas et al (2012) Tonic and transient endocannabinoid regulation of AMPAergic miniature postsynaptic currents and homeostatic plasticity in embryonic motor networks. PLoS One 32 13597. PMID: 23015449.

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