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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
分子量 | 307.35 |
公式 | C17H17N5O |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 LY 2183240 的部分引用包括:
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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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.