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Submit ReviewRo 60-0175 fumarate is a potent, selective 5-HT2 receptor agonist; shows selectivity for the 5-HT2C subtype (pKi values are 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively). Centrally active following oral or systemic administration in vivo.
Ro 60-0175 fumarate is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 342.75 |
公式 | C11H12ClFN2.C4H4O4 |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 169675-09-6 |
PubChem ID | 6446435 |
InChI Key | CEPHEXXZGQBXGT-XZTIXWOLSA-N |
Smiles | O=C(O)/C=C/C(O)=O.FC1=C(Cl)C=C(N(C[C@H](C)N)C=C2)C2=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 1.71 | 5 | |
DMSO | 6.86 | 20 |
以下数据基于产品分子量 342.75。 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 |
---|---|---|---|
0.2 mM | 14.59 mL | 72.94 mL | 145.88 mL |
1 mM | 2.92 mL | 14.59 mL | 29.18 mL |
2 mM | 1.46 mL | 7.29 mL | 14.59 mL |
10 mM | 0.29 mL | 1.46 mL | 2.92 mL |
参考文献是支持产品生物活性的出版物。
Damjanoska et al (2003) Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol-l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine2C receptor agonist. J.Pharmacol.Exp.Ther. 304 1209 PMID: 12604698
Kennett et al (2000) Effects of Ro 60 0175, a 5-HT2C receptor agonist, in three animal models of anxiety. Eur.J.Pharmacol. 387 197 PMID: 10650160
Martin et al (1998) 5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential. J.Pharmacol.Exp.Ther. 286 913 PMID: 9694950
Jensen et al (2013) Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT2A/5-HT2C receptor agonists with pro-cognitive J.Med.Chem. 56 1211 PMID: 23301527
If you know of a relevant reference for Ro 60-0175 fumarate, please let us know.
关键词: Ro 60-0175 fumarate, Ro 60-0175 fumarate supplier, Potent, selective, 5-HT2C, agonists, Serotonin, Receptors, Ro60-0175, 1854, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Ro 60-0175 fumarate 的部分引用包括:
Yu and Yamaguchi (2009) 5-HT2C-like receptors in the brain of Xenopus laevis initiate sex-typical fictive vocalizations. J Neurophysiol 102 752 PMID: 19474172
Craige and Unterwald (2013) Serotonin (2C) receptor regulation of cocaine-induced conditioned place preference and locomotor sensitization. Behav Brain Res 238 206 PMID: 23103406
Kawahara et al (2008) Dysregulated editing of serotonin 2C receptor mRNAs results in energy dissipation and loss of fat mass. J Neurosci 28 12834 PMID: 19036977
Mbaki (2008) Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anaesthetized female rat. Br J Pharmacol 155 343 PMID: 18604238
Manvich et al (2012) Effects of serotonin 2C receptor agonists on the behavioral and neurochemical effects of cocaine in squirrel monkeys. J Pharmacol Exp Ther 341 424 PMID: 22328576
Yu and Yamaguchi (2010) Endogenous serotonin acts on 5-HT2C-like receptors in key vocal areas of the brain stem to initiate vocalizations in Xenopus laevis. J Biol Chem 103 648 PMID: 19955293
Nagata et al (2019) Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic β-cells. Sci Rep 9 16438 PMID: 31712714
Martin et al (2015) 5-HT2C receptor desensitization moderates anxiety in 5-HTT deficient mice: from behavioral to cellular evidence. Synapse 18 PMID: 25522398
Kasper et al (2015) Serotonin-2C receptor agonists decrease potassium-stimulated GABA release in the nucleus accumbens. J Neurophysiol 69 78 PMID: 25382408
Martin et al (2014) Effect of genetic and pharmacological blockade of GABA receptors on the 5-HT2C receptor function during stress. J Neurochem 131 566 PMID: 25113583
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