SB 204741

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Cat.No. 1372 - SB 204741 | C14H14N4OS | CAS No. 152239-46-8
Description: Potent, selective 5-HT2B antagonist
Chemical Name: N-(1-Methyl-1H-indolyl-5-yl)-N''-(3-methyl-5-isothiazolyl)urea
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Literature

Biological Activity

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

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 28.64 100
ethanol 5.73 20

Preparing Stock Solutions

The following data is based on the product molecular weight 286.35. 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 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: SB 204741, supplier, Potent, selective, 5-HT2B, antagonists, Serotonin, Receptors, SB204741, 5-HT2B, Receptors, 5-HT2B, Receptors, Tocris Bioscience

4 Citations for SB 204741

Citations are publications that use Tocris products. Selected citations for SB 204741 include:

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

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

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

Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641


Do you know of a great paper that uses SB 204741 from Tocris? If so please let us know.

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