SB 204741

Catalog #: 1372
7 Citations Datasheet

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SB 204741 | CAS No. 152239-46-8 | 5-HT2B Receptor Antagonists

1 Image

Description: Potent, selective 5-HT2B antagonist

Chemical Name: N-(1-Methyl-1H-indolyl-5-yl)-N''-(3-methyl-5-isothiazolyl)urea

Purity: ≥99%

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Product Details

Citations (7)

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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

SB 204741 is a potent and selective 5-HT_2B receptor antagonist (pA₂ = 7.95). Displays ≥ 135-fold selectivity over 5-HT_2C (pK_i = 5.82), 5-HT_2A (pK_i < 5.2), 5-HT_1A, _1D, _1E, 5-HT₃ and 5-HT₄ receptors.

Technical Data

M.Wt:

286.35

Formula:

C₁₄H₁₄N₄OS

Solubility:

Soluble to 100 mM in DMSO and to 20 mM in ethanol

Purity:

≥99%

Storage:

Store at RT

CAS No:

152239-46-8

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.

Additional Information

Licensing Caveats:

Sold under license

Background References

Stimulating healthy tissue regeneration by targeting the 5-HT_2B receptor in chronic liver disease.
Ebrahimkhani et al.
Nat.Med., 2011;17:1668
N-(1-Methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT_2B receptor antagonist.
Forbes et al.
J.Med.Chem., 1995;38:855
The pharmacology and distribution of human 5-hydroxytryptamine_2B (5-HT_2B) receptor gene products: comparison with 5-HT_2A and 5-HT_2C receptors.
Bonhaus et al.
Br.J.Pharmacol., 1995;115:622
Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT_2B receptors.
Glusa and Pertz
Br.J.Pharmacol., 2000;130:692

Product Datasheets

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Citations for SB 204741

The citations listed below are publications that use Tocris products. Selected citations for SB 204741 include:

7 Citations: Showing 1 - 7

Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic β-cells.
Authors: Nagata Et al.
Sci Rep 2019;9:16438
Serotonin Improves High Fat Diet Induced Obesity in Mice.
Authors: Watanabe Et al.
PLoS One 2016;11:e0147143
Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels.
Authors: Salzer Et al.
Neuropharmacology 2016;110 (A):277
Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude.
Authors: Gerhold Et al.
J Neurosci 2015;35:9580
Mammary gland serotonin regulates parathyroid hormone-related protein and other bone-related signals.
Authors: Hernandez Et al.
BMC Complement Altern Med 2012;302:E1009
Protein kinase C{gamma} mediates regulation of proliferation by the serotonin 5-hydroxytryptamine receptor 2B.
Authors: Wouters Et al.
J Biol Chem 2009;284:21177
Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
Authors: Hampson Et al.
Diabetologia 2007;50:1743

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