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Submit ReviewSB 258719 hydrochloride
Description: Selective 5-HT7 antagonist
Chemical Name: 3-Methyl-N-[(1R)-1-methyl-3-(4-methyl-1-piperidinyl)propyl]-N-methylbenzenesulfonamide hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for SB 258719 hydrochloride
SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries for SB 258719 hydrochloride
SB 258719 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SB 258719 hydrochloride
| M. Wt | 374.97 |
| Formula | C18H30N2O2S.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1217674-10-6 |
| PubChem ID | 56972181 |
| InChI Key | UIZKHTBWJSUGOV-UNTBIKODSA-N |
| Smiles | O=S(C1=CC(C)=CC=C1)(N(C)[C@H](C)CCN2CCC(C)CC2)=O.Cl |
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 SB 258719 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 37.5 | 100 | |
| DMSO | 37.5 | 100 |
Preparing Stock Solutions for SB 258719 hydrochloride
The following data is based on the product molecular weight 374.97. 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 | 2.67 mL | 13.33 mL | 26.67 mL |
| 5 mM | 0.53 mL | 2.67 mL | 5.33 mL |
| 10 mM | 0.27 mL | 1.33 mL | 2.67 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
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Product Datasheets for SB 258719 hydrochloride
References for SB 258719 hydrochloride
References are publications that support the biological activity of the product.
Forbes et al (1998) (R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl)propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist. J.Med.Chem. 41 655 PMID: 9513592
Thomas et al (1998) Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br.J.Pharmacol. 124 1300 PMID: 9720804
Guscott et al (2003) The hypothermic effect of 5-CT in mice is mediated through the 5-HT7receptor. Neuropharmacology 44 1031 PMID: 12763096
If you know of a relevant reference for SB 258719 hydrochloride, please let us know.
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Keywords: SB 258719 hydrochloride, SB 258719 hydrochloride supplier, Selective, 5-HT7, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB258719, hydrochloride, GlaxoSmithKline, GSK, 2726, Tocris Bioscience
3 Citations for SB 258719 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 258719 hydrochloride include:
Johnson et al (2011) Serotonin receptor activity is necessary for olfactory learning and memory in Drosophila melanogaster. Neuroscience 192 372 PMID: 21749913
Domínguez-Soto (2017) Serotonin drives the acquisition of a profibrotic and anti-inflammatory gene profile through the 5-HT7R-PKA signaling axis. Sci Rep 7 14761 PMID: 29116249
Zhao et al (2015) Fisetin exerts antihyperalgesic effect in a mouse model of neuropathic pain: engagement of spinal serotonergic system. Front Synaptic Neurosci 5 9043 PMID: 25761874
Do you know of a great paper that uses SB 258719 hydrochloride 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.