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Submit ReviewRo 60-0175 fumarate
Description: Potent, selective 5-HT2C agonist
Chemical Name: (αS)-6-Chloro-5-fluoro-α-methyl-1H-indole-1-ethanamine fumarate
Purity: ≥98% (HPLC)
Biological Activity for Ro 60-0175 fumarate
Ro 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.
Compound Libraries for Ro 60-0175 fumarate
Ro 60-0175 fumarate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Ro 60-0175 fumarate
| M. Wt | 342.75 |
| Formula | C11H12ClFN2.C4H4O4 |
| Storage | Desiccate at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ro 60-0175 fumarate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 1.71 | 5 | |
| DMSO | 6.86 | 20 |
Preparing Stock Solutions for Ro 60-0175 fumarate
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for Ro 60-0175 fumarate
References for Ro 60-0175 fumarate
References are publications that support the biological activity of the product.
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.
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Keywords: Ro 60-0175 fumarate, Ro 60-0175 fumarate supplier, Potent, selective, 5-HT2C, agonists, Serotonin, Receptors, Ro60-0175, 1854, Tocris Bioscience
10 Citations for Ro 60-0175 fumarate
Citations are publications that use Tocris products. Selected citations for Ro 60-0175 fumarate include:
Craige and Unterwald (2013) Serotonin (2C) receptor regulation of cocaine-induced conditioned place preference and locomotor sensitization. Behav Brain Res 238 206 PMID: 23103406
Nagata et al (2019) Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic β-cells. Sci Rep 9 16438 PMID: 31712714
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
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
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
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
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
Do you know of a great paper that uses Ro 60-0175 fumarate from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.