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| WIN 55,212-2 MESYLATE Basic information |
| Product Name: | WIN 55,212-2 MESYLATE | | Synonyms: | (+)-WIN 55,212-2 mesylate - CAS 131543-23-2 - Calbiochem;CS-754;WIN552122;WIN-552122;R(+)-WIN 55,212-2 ,MESYLATE HIGH AFFINIT Y CANNABI;(R)-(+)-(2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1.2.3-de]-1,4-benzoxazin-6-yl)-1-naphthalenylmethanonemesy;212-2Mesylate;WIN55;(R)-(+)-[2,3-Dihydro-5-methyl-3[(4-morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate salt | | CAS: | 131543-23-2 | | MF: | C28H30N2O6S | | MW: | 522.62 | | EINECS: | 1592732-453-0 | | Product Categories: | Cannabinoid receptor;Cannabinoid | | Mol File: | 131543-23-2.mol |
| WIN 55,212-2 MESYLATE Chemical Properties |
| storage temp. | Store at +4°C | | solubility | 0.1 M HCl: 0.25 mg/mL | | form | solid | | color | white to off-white | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| WIN 55,212-2 MESYLATE Usage And Synthesis |
| Description | (+)-WIN 55,212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Ki values of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. In primary cultures of rat cerebral cortex neurons, (+)-WIN 55,212-2 (mesylate) (0.01-100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve. This effect is fully counteracted by rimonabant at a concentration of 10 nM, by decreasing Ca2+ concentrations below 0.2 mM, or by the IP3 receptor antagonist xestospongin C at a concentration of 1 μM. (+)-WIN 55,212-2 (mesylate) induces release of the proinflammatory neuropeptide CGRP from trigeminal ganglion (TG) neurons in a calcium-dependent manner with an EC50 value of 26 μM. | | Uses | (R)-(+)-WIN 55,212-2 mesylate salt has been used as a high affinity cannabinoid agonist for intraperitoneal injection into rats to induce behavioural sensitization. It has also been used as a synthetic cannabinoid drug and cannabinoid receptor 1 (CNR1) agonist to treat Becn2+/? mice and wild-type (WT) littermate to analyze the levels of CNR1 in the brain. | | General Description | WIN 55,212-2 is a member of the aminoalkylindole class of compounds. | | Biological Activity | Nanomolar affinity cannabinoid receptor agonist (K i values are 62.3 and 3.3 nM at the human cloned CB 1 and CB 2 receptors respectively). Also available as part of the Cannabinoid Receptor Agonist Tocriset™ . | | Biochem/physiol Actions | It is known to decrease the lipopolysaccharide mediated release of tumor necrosis factor- α and interleukin-1 in mice. | | References | 1) Felder?et al. (1995),?Comparison of the pharmacology and signal transduction of the human cannabinoid CB1?and CB2receptors; Mol. Pharmacol.,?48?443
2) Herzberg?et al. (1997),?The analgesic effects of R(+)-WIN 55,212-2 mesylate, a high affinity cannabinoid agonist in a rat model of neuropathic pain; Neurosci. Lett.,?221?157
3) Bouaboula?et al. (1995),?Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1; Biochem. J.,?312?637 |
| WIN 55,212-2 MESYLATE Preparation Products And Raw materials |
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