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Submit ReviewRS 39604 hydrochloride
Description: 5-HT4 antagonist
Chemical Name: 1-[4-Amino-5-chloro-2-(3,5-dimethoxyphenyl)methyloxy]-3-[1-[2-methylsulphonylamino]ethyl]piperidin-4-yl]propan-1-one hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for RS 39604 hydrochloride
RS 39604 hydrochloride is a potent and selective 5-HT4 antagonist, with a pKi of 9.1 at 5-HT4 receptors in guinea pig striatal membranes and greater than 1000-fold selectivity over 5-HT1A, 2C, 3 and D1, D2, M1, M2, AT1, B1 and α1C receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo studies.
Licensing Information
Sold with the permission of Roche Bioscience
Compound Libraries for RS 39604 hydrochloride
RS 39604 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for RS 39604 hydrochloride
| M. Wt | 590.56 |
| Formula | C26H36ClN3O6S.HCl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 167710-87-4 |
| PubChem ID | 19081934 |
| InChI Key | QSMYZGMJSGUWPM-UHFFFAOYSA-N |
| Smiles | Cl.COC1=CC(OC)=CC(COC2=CC(N)=C(Cl)C=C2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)=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 RS 39604 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 59.06 | 100 |
Preparing Stock Solutions for RS 39604 hydrochloride
The following data is based on the product molecular weight 590.56. 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 |
|---|---|---|---|
| 1 mM | 1.69 mL | 8.47 mL | 16.93 mL |
| 5 mM | 0.34 mL | 1.69 mL | 3.39 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.69 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets for RS 39604 hydrochloride
References for RS 39604 hydrochloride
References are publications that support the biological activity of the product.
Eglen et al (1995) Central 5-HT4 receptors TiPS 16 391 PMID: 8578609
Hegde (1995) RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist. Br.J.Pharmacol. 115 1087 PMID: 7582507
If you know of a relevant reference for RS 39604 hydrochloride, please let us know.
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Keywords: RS 39604 hydrochloride, RS 39604 hydrochloride supplier, 5-HT4, antagonist, Serotonin, Receptors, 5-Hydroxytryptamine, RS39604, hydrochloride, 0991, Tocris Bioscience
3 Citations for RS 39604 hydrochloride
Citations are publications that use Tocris products. Selected citations for RS 39604 hydrochloride include:
Müller et al (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One 4 e6453 PMID: 19649285
Ratner et al (2012) Cerebral markers of the serotonergic system in rat models of obesity and after Roux-en-Y gastric bypass. Learn Mem 20 2133 PMID: 22450706
Huang and Kandel (2007) Low-frequency stimulation induces a pathway-specific late phase of LTP in the amygdala that is mediated by PKA and dependent on protein synthesis. J Pharmacol Exp Ther 14 497 PMID: 17626908
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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.