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Submit Review(±)-U-50488 hydrochloride
说明： Selective κ agonist
化学名： trans-(±)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide hydrochloride
纯度： ≥99% (HPLC)
生物活性 for (±)-U-50488 hydrochloride
(±)-U-50488 hydrochloride is a selective κ-opioid agonist. At higher concentrations blocks Na+ channels.
(-)-enantiomer and (+)-enantiomer also available.
技术数据 for (±)-U-50488 hydrochloride
| 分子量 | 405.79 |
| 公式 | C19H26Cl2N2O.HCl |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 67197-96-0 |
| PubChem ID | 90479733 |
| InChI Key | SKWPJQQGGZWRSK-PXOXCKTNSA-N |
| Smiles | O=C(CC3=CC(Cl)=C(Cl)C=C3)N([C@H]1[C@H](N2CCCC2)CCCC1)C.O=C(CC6=CC(Cl)=C(Cl)C=C6)N([C@@H]4[C@@H](N5CCCC5)CCCC4)C.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for (±)-U-50488 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 10.14 | 25 |
制备储备液 for (±)-U-50488 hydrochloride
以下数据基于产品分子量 405.79。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 9.86 mL | 49.29 mL | 98.57 mL |
| 1.25 mM | 1.97 mL | 9.86 mL | 19.71 mL |
| 2.5 mM | 0.99 mL | 4.93 mL | 9.86 mL |
| 12.5 mM | 0.2 mL | 0.99 mL | 1.97 mL |
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产品说明书 for (±)-U-50488 hydrochloride
参考文献 for (±)-U-50488 hydrochloride
参考文献是支持产品生物活性的出版物。
Pao-Luh Tao et al (1994) U-50,488 blocks the development of mor. tolerance and dependence at a very low dose in guinea pigs. Eur.J.Pharmacol. 256 281 PMID: 8045272
Suarez-Roca and Maixner (1993) Activation of kappa opioid receptors by U-50488H and mor. enhances the release of substance P from rat trigeminal nucleus slices. J.Pharmacol.Exp.Ther. 264 648 PMID: 7679733
Pugsley et al (1992) Cardiovascular actions of the κ-agonist, U-50-488H, in the absence and presence of opioid receptor blockade. Br.J.Pharmacol. 105 521 PMID: 1320979
Su et al (1998) Blockade of the development of mor. tolerance by U-50,488, an AVP antagonist or MK 801 in the rat hippocampal slice. Br.J.Pharmacol. 123 625 PMID: 9517380
If you know of a relevant reference for (±)-U-50488 hydrochloride, please let us know.
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关键词: (±)-U-50488 hydrochloride, (±)-U-50488 hydrochloride supplier, selective, agonists, κ-opioid, kappa-opioid, KOP, Receptors, OP2, Kappa, Opioid, 0495, Tocris Bioscience
9 篇 (±)-U-50488 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 (±)-U-50488 hydrochloride 的部分引用包括：
Dziedowiec et al (2018) sMu opioid receptor agonist DAMGO produces place conditioning, abstinence-induced withdrawal, and naltrexone-dependent locomotor activation in planarians. Neuroscience 386 214 PMID: 29958944
Liu (2018) In vivo brain GPCR signaling elucidated by phosphoproteomics. Science 360 eaao4927 PMID: 29930108
Grachev et al (2012) GPR54-dependent stimulation of luteinizing hormone secretion by neurokinin B in prepubertal rats. Pain 7 e44344 PMID: 23028524
Pirino et al (2020) Kappa-opioid receptor-dependent changes in dopamine and anxiety-like or approach-avoidance behavior occur differentially across the nucleus accumbens shell rostro-caudal axis Neuropharmacology 181 108341 PMID: 33011200
Zhou et al (2013) Development of functionally selective, small molecule agonists at kappa opioid receptors. J Biol Chem 288 36703 PMID: 24187130
Kharmate et al (2013) Inhibition of tumor promoting signals by activation of SSTR2 and opioid receptors in human breast cancer cells. Cancer Cell Int 13 93 PMID: 24059654
Polter (2017) Constitutive activation of kappa opioid receptors at ventral tegmental area inhibitory synapsesfollowing acute stress Elife 6 e23785 PMID: 28402252
Li et al (2019) Kappa opioid receptor agonists improve postoperative cognitive dysfunction in rats via the JAK2/STAT3 signaling pathway. Int J Mol Med PMID: 31545485
Marchant et al (2010) Medial dorsal hypothalamus mediates the inhibition of reward seeking after extinction. J Neurosci 30 14102 PMID: 20962231
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Beta arrestin recruitment.
By
Anonymous on 06/15/2021
分析类型： In Vitro
种属： Human
Dose response curve of beta arrestin recruitment (Presto_Tango assay)
JNK-dependent rescue of LTPGABA by acute norBNI.
By
Anonymous on 03/18/2020
分析类型： In Vivo
种属： Rat
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U50488 (5 mg/kg) injection
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By
Anonymous on 03/05/2020
分析类型： In Vitro
种属： Human
细胞系/组织： CHO
Successfully induced ERK1/2 phosphorylation in CHO cells expressing KOR.
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By
Matthew Banks on 01/05/2018
分析类型： In Vivo
种属： Rat
To evaluate the behavioral effects of unbiased and biased kappa agonists in animals
soluble in water up to 5.6 mg/mL
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