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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.
Sold under license from Eli Lilly and Company
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||15.37||50 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 307.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.25 mL||16.27 mL||32.54 mL|
|5 mM||0.65 mL||3.25 mL||6.51 mL|
|10 mM||0.33 mL||1.63 mL||3.25 mL|
|50 mM||0.07 mL||0.33 mL||0.65 mL|
References are publications that support the biological activity of the product.
Dickason-Chesterfield et al (2006) Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol.Neurobiol. 26 407 PMID: 16736384
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
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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Keywords: LY 2183240, LY 2183240 supplier, FAAH, inhibitors, inhibits, anandamide, reuptake, potent, Anandamide, Amidase, Fatty, Acid, Amide, Hydrolases, AMT, Transporters, cannabinoids, Monoamine, Neurotransmitter, LY2183240, Cannabinoid, Hydrolase, (FAAH), Other, Cannabinoids, 2452, Tocris Bioscience
1 Citation for LY 2183240
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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