Biological Activity
Potent and selective 5-HT4 receptor antagonist (pIC50 = 10.1). Displays >5000-fold selectivity for 5-HT4 over 5-HT1A, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2C, and 5-HT3 receptors. Exhibits anxiolytic activity upon systemic administration in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data
| M. Wt | 419.34 |
| Formula | C19H27ClN2O4.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 148688-01-1 |
| PubChem ID | 121880 |
| InChI Key | YEQGKAOSYSXEPU-UHFFFAOYSA-N |
| Smiles | ClC1=C(N)C(OCCO2)=C2C(C(OCC3CCN(CCCC)CC3)=O)=C1.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 | 41.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 419.34. 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 | 2.38 mL | 11.92 mL | 23.85 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bingham et al (1995) Antagonism by SB 204070 of 5-HT-evoked contractions in the dog stomach: an in-vivo model of 5-HT4 receptor function. J.Pharm.Pharmacol. 47 219 PMID: 7602484
Gaster et al (1993) (1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 antagonist derived from metoclopramide. J.Med.Chem. 36 4121 PMID: 8258837
Prins et al (2000) An improved in vitro bioassay for the study of 5-HT4 receptors in the human isolated large intestine circular muscle. Br.J.Pharmacol. 129 1601 PMID: 10780964
Keywords: SB 204070, supplier, Serotonin, serotonergics, selective, 5-HT4, receptors, antagonists, anxiolytics, SB204070, 5-HT4, Receptors, 5-HT4, Receptors, Tocris Bioscience
