L9044
LY2183240
≥98% (HPLC)
Synonym(s):
1H-Tetrazole-1-carboxamide, 5-([1,1′-biphenyl]-4-ylmethyl)-N,N-dimethyl-, 5-Biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide
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About This Item
Empirical Formula (Hill Notation):
C17H17N5O
CAS Number:
Molecular Weight:
307.35
UNSPSC Code:
12352200
MDL number:
assay
≥98% (HPLC)
drug control
Új pszichoaktív anyag / New psychoactive substance (Hungary), 78/2022. (XII. 28.) BM rendelet
storage condition
desiccated
solubility
DMSO: >10 mg/mL
storage temp.
2-8°C
SMILES string
CN(C)C(=O)n1nnnc1Cc2ccc(cc2)-c3ccccc3
Biochem/physiol Actions
Regioisomer 1-5 of LY2183240 is a potent inhibitor of anandamide uptake (IC50= 15 nM).
Regioisomer 1-5 of LY2183240 is a potent inhibitor of anandamide uptake (IC50= 15 nM). The compound inhibits FAAH (IC50=2.1 nM) and some other brain serine proteases. After systemic administration to rodents, LY2182340 elevates brain anandamide levels and shows efficacy in a rodent model of persistent pain (ED50=1.37 mg/kg). Regioisomer 2-5 of LY2183240 is less active. The compound is more potent than N-(4-Hydroxyphenyl)-arachidonylamide (AM-404), which inhibits anandamide transport at IC50=1mM.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Simon Nicolussi et al.
Biochemical pharmacology, 92(4), 669-689 (2014-10-07)
Besides the suggested role of a putative endocannabinoid membrane transporter mediating the cellular uptake of the endocannabinoid anandamide (AEA), this process is intrinsically coupled to AEA degradation by the fatty acid amide hydrolase (FAAH). Differential blockage of each mechanism is