WIN 55,212-2メシル酸塩 化学特性,用途語,生産方法
外観
白色〜黄褐色, 結晶〜粉末
溶解性
N,N-ジメチルホルムアミド溶状:試験適合
説明
(+)-WIN 55,212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with K
i values of 62.3 and 3.3 nM for human recombinant CB
1 and CB
2 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 Ca
2+ concentrations below 0.2 mM, or by the IP
3 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 EC
50 value of 26 μM.
使用
(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.
一般的な説明
WIN 55,212-2 is a member of the aminoalkylindole class of compounds.
生物活性
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™ .
WIN 55,212-2メシル酸塩 上流と下流の製品情報
原材料
準備製品