VDM-11

BML-CR111

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Anandamide transporter inhibitor

Selective and potent inhibitor of the anandamide membrane transporter (AMT) (neuronal (C6 glioma cells): IC₅₀=11µM; non-neuronal (rat RBL-2H3 cells): IC₅₀=7.2µM) with negligible action at TRPV1 and weak action at CB₁ receptor (CB₁: K_i=5µM; CB₂: K_i>5µM) and FAAH (IC₅₀=3.7µM/ IC₅₀>50µM (N18TG2 cell membranes).

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Product Details

Alternative Name	N-Arachidonoyl-4-hydroxy-2-methylaniline, N-(4-Hydroxy-2-methylphenyl)arachidonoylamide
Appearance	Tan oil.
CAS	313998-81-1
Couple Target	Anandamide transporter
Couple Type	Inhibitor
Formula	C₂₇H₃₉NO₂
MW	409.6
Purity	≥98% (TLC)
Solubility	Soluble in DMSO (1.5mg/ml) or ethanol (1mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C.
Handling	Keep under inert gas.
Long Term Storage	-20°C
Shipping	Dry Ice

Regulatory Status	RUO – Research Use Only

Characterization of an anandamide degradation system in prostate epithelial PC-3 cells: synthesis of new transporter inhibitors as tools for this study: L. Ruiz-Llorente et al.; Br. J. Pharmacol. 141, 457 (2004), Abstract
Endocannabinoids as physiological regulators of colonic propulsion in mice: L. Pinto, et al.; Gastroenterology 123, 227 (2002), Abstract
Experimental parkinsonism alters endocannabinoid degradation: implications for striatal glutamatergic transmission: P. Gubellini, et al.; J. Neurosci. 22, 6900 (2002), Abstract
Endocannabinoids control spasticity in a multiple sclerosis model: D. Baker, et al.; FASEB J. 15, 300 (2001), Abstract — Full Text
Exogenous anandamide protects rat brain against acute neuronal injury in vivo: M. van der Stelt, et al.; J. Neurosci. 21, 8765 (2001), Abstract
The activity of anandamide at vanilloid VR1 receptors requires facilitated transport across the cell membrane and is limited by intracellular metabolism: L. De Petrocellis, et al.; J. Biol. Chem. 276, 12856 (2001), Abstract — Full Text
Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity: L. De Petrocellis, et al.; FEBS Lett. 483, 52 (2000), Abstract

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VDM-11

BML-CR111

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