(±)-U-50488 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
(±)-U-50488 hydrochloride是κ阿片受体的选择性激动剂[1]。
κ阿片受体(KOR)是阿片肽强啡肽的阿片受体,参与控制成瘾。此外,KOR在紧张、焦虑、快感缺乏、抑郁症和寻求药物行为增加中发挥重要的作用。
(±)-U-50488 hydrochloride是KOR的选择性激动剂[1]。在离体大鼠DRG神经元中,0.3-40 μM 的U-50488抑制电压不依赖性的钙离子通道电流。在不表达KOR的HeLa细胞中,20 μM的U-50488阻断钙通道[2]。
在恒河猴中,U-50488显示出强效的镇痛活性和利尿作用[1]。U-50488增强电刺激诱导的兔输精管收缩,IC50值为26.5 nM。在小鼠中,U-50488损坏运动功能,降低自发性活动,ED50值为15.3 mg/kg[3]。在成年大鼠中,U-50488增加维持自我刺激响应所需要的阈值,产生抑郁样效果。同时,与女性相比,男性对阈值增加的效应更加敏感[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.
Physical Appearance | White solid |
Storage | Desiccate at RT |
M.Wt | 405.79 |
Cas No. | 67197-96-0 |
Formula | C19H26Cl2N2O·HCl |
Solubility | <10.14mg/ml in H2O |
Chemical Name | 2-(3,4-dichlorophenyl)-N-methyl-N-((1R,2R)-2-(pyrrolidin-1-yl)cyclohexyl)acetamide hydrochloride |
SDF | Download SDF |
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 | 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。 |