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Submit ReviewSB 204741
说明： Potent, selective 5-HT2B antagonist
化学名： N-(1-Methyl-1H-indolyl-5-yl)-N''-(3-methyl-5-isothiazolyl)urea
纯度： ≥99% (HPLC)
生物活性 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.
许可信息
Sold under license
化合物库 for SB 204741
SB 204741 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for SB 204741
| 分子量 | 286.35 |
| 公式 | C14H14N4OS |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SB 204741
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 28.64 | 100 | |
| ethanol | 5.73 | 20 |
制备储备液 for SB 204741
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for SB 204741
参考文献 for SB 204741
参考文献是支持产品生物活性的出版物。
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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关键词: SB 204741, SB 204741 supplier, Potent, selective, 5-HT2B, antagonists, Serotonin, Receptors, SB204741, 1372, Tocris Bioscience
7 篇 SB 204741 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SB 204741 的部分引用包括：
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
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
Watanabe et al (2016) Serotonin Improves High Fat Diet Induced Obesity in Mice. PLoS One 11 e0147143 PMID: 26766570
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.