Replaces Prod. #: ALX-340-046
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: Ki=5µM; CB2: Ki>5µM) and FAAH (IC50=3.7µM/ IC50>50µM (N18TG2 cell membranes).
Product Details
Alternative Name: | N-Arachidonoyl-4-hydroxy-2-methylaniline, N-(4-Hydroxy-2-methylphenyl)arachidonoylamide |
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Formula: | C27H39NO2 |
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MW: | 409.6 |
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CAS: | 313998-81-1 |
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Purity: | ≥98% (TLC) |
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Appearance: | Tan oil. |
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Solubility: | Soluble in DMSO (1.5mg/ml) or ethanol (1mg/ml). |
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Shipping: | Dry Ice |
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Long Term Storage: | -20°C |
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Use/Stability: | 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. |
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Handling: | Keep under inert gas. |
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Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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.
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Endocannabinoids as physiological regulators of colonic propulsion in mice: L. Pinto, et al.; Gastroenterology
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Experimental parkinsonism alters endocannabinoid degradation: implications for striatal glutamatergic transmission: P. Gubellini, et al.; J. Neurosci.
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Endocannabinoids control spasticity in a multiple sclerosis model: D. Baker, et al.; FASEB J.
15, 300 (2001),
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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;