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N-Arachidonoyl-serotonin

TRPV1 antagonist
 
BML-VR106-0010 10 mg 84.00 USD
 
BML-VR106-0050 50 mg 284.00 USD
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Replaces Prod. #: ALX-340-060

Unnatural fatty acid-neurotransmitter conjugate. Potent TRPV1 antagonist (IC50=40nM). Inhibits fatty acid amide hydrolase (FAAH) (IC50=5.6mM). Enhances levels of anandamide and 2-AG in vivo. Displays analgesic activity in both acute and chronic peripheral pain models but shows little efficacy in an inflammatory bowel disease model.

Product Specification

Formula:C30H42N2O2
 
MW:462.7
 
CAS:187947-37-1
 
Purity:≥98% (TLC)
 
Appearance:Pale yellow oil.
 
Solubility:Soluble in DMSO (>25mg/ml), 100% ethanol (15mg/ml) or dimethyl formamide (30mg/ml); also soluble in PBS, pH 7.2 (290µg/ml).
 
Shipping:Shipped on Dry Ice
 
Long Term Storage:-20°C
 
Use/Stability:Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
 
Handling:Protect from air.
 
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Product Literature References

Analgesic actions of N-arachidonoyl-serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors: S. Maione, et al.; Br. J. Pharmacol. 150, 766 (2007), Abstract;
Up-regulation of anandamide levels as an endogenous mechanism and a pharmacological strategy to limit colon inflammation: G. D'Argenio, et al.; FASEB J. 20, 568 (2006), Abstract;
Effect of repeated systemic administration of selective inhibitors of endocannabinoid inactivation on rat brain endocannabinoid levels: E. de Lago, et al.; Biochem. Pharmacol. 70, 446 (2005), Abstract;
Arachidonoylserotonin and other novel inhibitors of fatty acid amide hydrolase: T. Bisogno, et al.; BBRC 248, 515 (1998), Abstract;

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