10009023  WIN 55212-2 (mesylate)

(CAS 131543-23-2)

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WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 3.3 and 62.3 nM for human recombinant CB1 and CB2 receptors, respectively.1 In primary cultures of rat cerebral cortex neurons, WIN 55212-2 (mesylate) (0.01-100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve.2 This effect at a concentration of 1 nM was fully counteracted by SR141716A (10 nM), by decreasing Ca2+ concentrations below 0.2 mM, and by the IP3 receptor antagonist xestospongin C at 1 µM. WIN 55212-2 (mesylate) induces release of the proinflammatory neuropeptide CGRP from trigeminal ganglion (TG) neurons in a calcium-dependent manner with an EC50 of 26 µM.3 In addition, WIN 55212-2 (mesylate)-evoked CGRP release is not stereospecific, as the CB receptor-inactive enantiomer WIN 55212-3 also stimulates CGRP exocytosis.
1  Felder, C.C., Joyce, K.E., Briley, E.M., et al. Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors. Mol Pharmacol 48 443-450 (1995).
2  Ferraro, L., Tomasini, C., Gessa, G.L., et al. The cannabinoid receptor agonist WIN 55,212-2 regulates glutamate transmission in rat cerebral cortex: An in vivo and in vitro study. Cerebral Cortex 11 728-733 (2001).
3  Price, T.J., Patwardhan, A., Akopian, A.N., et al. Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons. Br J Pharmacol 142 257-266 (2004).


Purchase 10009023 WIN 55212-2 (mesylate)

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Warning This product is not for human or veterinary use.

Pricing updated 2010-03-14.
Prices are subject to change without notice.

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.

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