| CAS NO: | 114528-81-3 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | White solid |
| Storage | Store at RT |
| M.Wt | 405.79 |
| Cas No. | 114528-81-3 |
| Formula | C19H26Cl2N2O·HCl |
| Solubility | <40.58mg/ml in DMSO;<40.58mg/ml in H2O |
| Chemical Name | 2-(3,4-dichlorophenyl)-N-methyl-N-((1R,2R)-2-(pyrrolidin-1-yl)cyclohexyl)acetamide hydrochloride |
| Canonical SMILES | CN(C(CC1=CC(Cl)=C(Cl)C=C1)=O)[C@]2([H])CCCC[C@@]2([H])N3CCCC3.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
(+)-U-50488 hydrochloride是一种作用于κ阿片受体的选择性激动剂[1].
κ阿片受体(KOR)是一类针对阿片肽强啡肽的阿片受体,控制成瘾.此外,KOR在紧张\焦虑\快感缺乏\抑郁症和增加药物寻求行为中起重要作用.
(+)-U-50488 hydrochloride是一种选择性的KOR激动剂[1].在离体大鼠DRG神经元中,U-50488(0.340 μM)抑制电压非依赖性Ca2+通道电流.在不表达KOR的HeLa细胞中,U-50488(20 μM)阻断Ca2+通道[2].
在恒河猴中,U-50488显示出强效的镇痛作用并产生利尿作用[1].U-50488增强电诱导的兔输精管收缩,IC50值为26.5 nM.在小鼠中,U-50488损害运动功能, ED50值为15.3 mg/kg,并降低自发性活动[3].在成年大鼠中,U-50488增加保持自我刺激响应(抑郁样效果)所需要的阈值.同时,男性对阈值增加的效应比女性更加敏感[4].
参考文献：
[1]. Tang AH, Collins RJ. Behavioral effects of a novel kappa opioid analgesic, U-50488, in rats and rhesus monkeys. Psychopharmacology (Berl), 1985, 85(3): 309-314.
[2]. Hassan B, Ruiz-Velasco V. The κ-opioid receptor agonist U-50488 blocks Ca2+ channels in a voltage- and G protein-independent manner in sensory neurons. Reg Anesth Pain Med, 2013, 38(1): 21-27.
[3]. Lu SN, Ma SC, Zhang KG, et al. Comparison of pharmacological profile of selective kappa-opioid agonist K-II and U-50488. Yao Xue Xue Bao, 1991, 26(3): 171-174.
[4]. Russell SE, Rachlin AB, Smith KL, et al. Sex differences in sensitivity to the depressive-like effects of the kappa opioid receptor agonist U-50488 in rats. Biol Psychiatry, 2014, 76(3): 213-222.
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