Biological Activity
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
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.5 | 100 | |
| ethanol | 37.5 | 100 | |
| water | 37.5 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 374.97. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
Keywords: SB 258719 hydrochloride, supplier, Selective, 5-HT7, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB258719, hydrochloride, GlaxoSmithKline, GSK, 5-HT7, Receptors, 5-HT7, Receptors, Tocris Bioscience
