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Activator of CB1 receptor and TRPV1
BML-VR100-0025 25 mg 217.00 USD
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Replaces Prod. #: ALX-340-041

A vanilloid agonist which is 10-fold more potent than capsaicin. "Hybrid" activator of CB1 receptor (CB1: Ki=1.6µM; CB2: Ki=15µM) and TRPV1 (Ki=0.4µM; EC50=33nM (human); EC50=6.71nM (rat)). Also inhibits anandamide uptake (IC50=9µM, Ki=14.1µM) and fatty acid amide hydrolase (FAAH) (IC50=20µM).

Product Specification

Alternative Name:NE-19550, N-Vanillyloleoylamide
Purity:≥98% (TLC)
Appearance:White to off-white solid.
Solubility:Soluble in DMSO (>25mg/ml).
Shipping:Shipped on Blue Ice
Long Term Storage:-20°C
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.
BML-VR100 structure
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BML-VR100 structure

Product Literature References

Effects of the vanilloid agonist olvanil and antagonist capsazepine on rat behaviors: J.W. Kasckow, et al.; Prog. Neuropsychopharmacol. Biol. Psychiatry 28, 291 (2004), Abstract;
Identification of species-specific determinants of the action of the antagonist capsazepine and the agonist PPAHV on TRPV1: E. Phillips, et al.; J. Biol. Chem. 279, 17165 (2004), Abstract;
Evidence against the presence of an anandamide transporter: S.T. Glaser, et al.; PNAS 100, 4269 (2003), Abstract;
Characterisation using FLIPR of human vanilloid VR1 receptor pharmacology: D. Smart et al.; Eur. J. Pharmacol. 417, 51 (2001), Abstract;
Characterization using FLIPR of rat vanilloid receptor (rVR1) pharmacology: J.C. Jerman, et al.; Br. J. Pharmacol. 130, 916 (2000), Abstract;
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;
Anandamide transport inhibition by the vanilloid agonist olvanil: M. Beltramo & D. Piomelli; Eur. J. Pharmacol. 364, 75 (1999), Abstract;
The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons: A. Szallasi et al.; Mol. Pharmacol. 56, 581 (1999), Abstract;
Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors: D. Melck, et al.; BBRC 262, 275 (1999), Abstract;
Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide: P.M. Zygmunt, et al.; Nature 400, 452 (1999), Abstract;
Interactions between synthetic vanilloids and the endogenous cannabinoid system: V. Di Marzo, et al.; FEBS Lett. 436, 449 (1998), Abstract;
Olvanil: more potent than capsaicin at stimulating the efferent function of sensory nerves: S.R. Hughes, et al.; Eur. J. Pharmacol. 219, 481 (1992), Abstract;
The antinociceptive effect and pharmacokinetics of olvanil following oral and subcutaneous dosing in the mouse: W.K. Sietsema, et al.; Life Sci. 43, 1385 (1988), Abstract;
NE-19550: a novel, orally active anti-inflammatory analgesic: L. Brand, et al.; Drugs Exp. Clin. Res. 13, 259 (1987), Abstract;

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