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LY 2183240

Catalog #: 2452
1 Citation Datasheet / COA / SDS

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2452 has been discontinued.
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LY 2183240 | CAS No. 874902-19-9 | Cannabinoid Transporter Inhibitors
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Description: Highly potent anandamide uptake inhibitor; also inhibits FAAH

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

Purity: ≥98%

Product Details
Citations (1)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

LY 2183240 is a 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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under license from Eli Lilly and Company

Background References

  1. Evidence for bidirectional endocannabinoid transport across cell membranes.
    Chicca A, Marazzi J, Nicolussi S, Gertsch J
    J Biol Chem, 2012;287(41):34660-82.
  2. Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors.
    Dickason-Chesterfield et al.
    Cell Mol.Neurobiol., 2006;26:407
  3. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases.
    Alexander and Cravat
    J.Am.Chem.Soc., 2006;128:9699
  4. Identification of a high-affinity binding site involved in the transport of endocannabinoids.
    Moore et al.
    Proc.Natl.Acad.Sci.USA, 2005;102:17852

Product Datasheets

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Citation for LY 2183240

The citations listed below are publications that use Tocris products. Selected citations for LY 2183240 include:

1 Citation: Showing 1 - 1

  1. Tonic and transient endocannabinoid regulation of AMPAergic miniature postsynaptic currents and homeostatic plasticity in embryonic motor networks.
    Authors: Gonzalez-Islas Et al.
    PLoS One  2012;32:13597

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