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Description: Potent, selective 5-HT2B antagonist
Chemical Name: N-(1-Methyl-1H-indolyl-5-yl)-N''-(3-methyl-5-isothiazolyl)urea
Purity: ≥99% (HPLC)
Biological Activity for SB 204741
SB 204741 is a potent and selective 5-HT2B receptor antagonist (pA2 = 7.95). Displays ≥ 135-fold selectivity over 5-HT2C (pKi = 5.82), 5-HT2A (pKi < 5.2), 5-HT1A, 1D, 1E, 5-HT3 and 5-HT4 receptors.
Licensing Information
Sold under license
Compound Libraries for SB 204741
SB 204741 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SB 204741
| M. Wt | 286.35 |
| Formula | C14H14N4OS |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 152239-46-8 |
| PubChem ID | 3277600 |
| InChI Key | USFUFHFQWXDVMH-UHFFFAOYSA-N |
| Smiles | O=C(NC3=CC(C)=NS3)NC1=CC(C=CN2C)=C2C=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 SB 204741
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.64 | 100 | |
| ethanol | 5.73 | 20 |
Preparing Stock Solutions for SB 204741
The following data is based on the product molecular weight 286.35. 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 | 3.49 mL | 17.46 mL | 34.92 mL |
| 5 mM | 0.7 mL | 3.49 mL | 6.98 mL |
| 10 mM | 0.35 mL | 1.75 mL | 3.49 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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Product Datasheets for SB 204741
References for SB 204741
References are publications that support the biological activity of the product.
Bonhaus et al (1995) The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. Br.J.Pharmacol. 115 622 PMID: 7582481
Forbes et al (1995) N-(1-Methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist. J.Med.Chem. 38 855 PMID: 7699699
Glusa and Pertz (2000) Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors. Br.J.Pharmacol. 130 692 PMID: 10821800
Ebrahimkhani et al (2011) Stimulating healthy tissue regeneration by targeting the 5-HT2B receptor in chronic liver disease. Nat.Med. 17 1668 PMID: 22120177
If you know of a relevant reference for SB 204741, please let us know.
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Keywords: SB 204741, SB 204741 supplier, Potent, selective, 5-HT2B, antagonists, Serotonin, Receptors, SB204741, 1372, Tocris Bioscience
7 Citations for SB 204741
Citations are publications that use Tocris products. Selected citations for SB 204741 include:
Watanabe et al (2016) Serotonin Improves High Fat Diet Induced Obesity in Mice. PLoS One 11 e0147143 PMID: 26766570
Salzer et al (2016) Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels. Neuropharmacology 110 (A) 277 PMID: 27511837
Hernandez et al (2012) Mammary gland serotonin regulates parathyroid hormone-related protein and other bone-related signals. BMC Complement Altern Med 302 E1009 PMID: 22318950
Nagata et al (2019) Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic β-cells. Sci Rep 9 16438 PMID: 31712714
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641
Wouters et al (2009) Protein kinase C{gamma} mediates regulation of proliferation by the serotonin 5-hydroxytryptamine receptor 2B. J Biol Chem 284 21177 PMID: 19531484
Do you know of a great paper that uses SB 204741 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.