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N-Arachidonoyl-serotonin

BML-VR106

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TRPV1 antagonist

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.

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Product Details

Appearance	Pale yellow oil.
CAS	187947-37-1
Couple Target	FAAH, TRP channel
Couple Type	Blocker, Inhibitor
Formula	C₃₀H₄₂N₂O₂
MW	462.7
Purity	≥98% (TLC)
Solubility	Soluble in DMSO (>25mg/ml), 100% ethanol (15mg/ml) or dimethyl formamide (30mg/ml); also soluble in PBS, pH 7.2 (290µg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. 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.
Long Term Storage	-20°C
Shipping	Dry Ice

Regulatory Status	RUO – Research Use Only

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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N-Arachidonoyl-serotonin

BML-VR106

Product Details

Handling & Storage

Datasheet, Manuals, SDS & CofA

Manuals And Inserts

Certificate of Analysis

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