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Submit ReviewLY 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.
Sold under license from Eli Lilly and Company
M. Wt | 307.35 |
Formula | C17H17N5O |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 874902-19-9 |
PubChem ID | 11507802 |
InChI Key | GZNIYOXWFCDBBJ-UHFFFAOYSA-N |
Smiles | CN(C)C(=O)N1N=NN=C1CC1=CC=C(C=C1)C1=CC=CC=C1 |
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.
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
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
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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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.