A-836339

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Chemical Structure| 959746-77-1 同义名 : -
CAS号 : 959746-77-1
货号 : A409715
分子式 : C16H26N2O2S
纯度 : 98+%
分子量 : 310.45
MDL号 : MFCD17167006
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(38.65 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 A-836339 is a potent and selective CB(2) agonist. A-836339 displays high affinities at CB(2) receptors and selectivity over CB(1) receptors in both human and rat. In addition A-836339 exhibits a profile devoid of significant affinity at other G-protein-coupled receptors and ion channels. A-836339 has also demonstrated efficacies in the chronic constrain injury (CCI) model of neuropathic pain, skin incision, and capsaicin-induced secondary mechanical hyperalgesia models[3]. Systemic administration of A-836339 (0.3-3 micromol/kg, i.v.) reduced both evoked and spontaneous WDR (wide dynamic range) neuronal activity in neuropathic, but not sham rats. Similar to systemic delivery, intra-spinal injection of A-836339 (0.3 and 1 nmol) also attenuated both von Frey-evoked and spontaneous firing of WDR neurons in neuropathic rats. Application of A-836339 (3-30 nmol) onto the ipsilateral L5 dorsal root ganglion (DRG) of neuropathic rats reduced the von Frey-evoked activity of WDR neurons, but spontaneous firing was unaltered[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.11mL

3.22mL

1.61mL

32.21mL

6.44mL

3.22mL
参考文献

[1]McGaraughty S, Chu KL, et al. A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors. Neuroscience. 2009 Feb 18;158(4):1652-61.

[2]Yao BB, Hsieh G, et al. Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene] -amide] , using in vitro pharmacological assays, in vivo pain models, and pharmacological magnetic resonance imaging. J Pharmacol Exp Ther. 2009 Jan;328(1):141-51.

[3]Yao BB, Hsieh G, Daza AV, et al. Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pain models, and pharmacological magnetic resonance imaging. J Pharmacol Exp Ther. 2009;328(1):141-151

[4]McGaraughty S, Chu KL, Dart MJ, Yao BB, Meyer MD. A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors. Neuroscience. 2009;158(4):1652-1661