SB 204741

Pricing Availability   Qty
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 (7)
Reviews
Literature (2)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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


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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:

Nagata et al (2019) Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic β-cells. Sci Rep 9 16438 PMID: 31712714

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

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


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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

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

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.