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Submit ReviewSB 206553 hydrochloride
说明： Potent and selective 5-HT2B and 5-HT2C antagonist; orally active
化学名： 3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide hydrochloride
纯度： ≥99% (HPLC)
生物活性 for SB 206553 hydrochloride
SB 206553 hydrochloride is a potent and selective 5-HT2B/5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92). Displays > 80-fold selectivity over all other 5-HT receptor subtypes and a variety of other receptors (pKi < 6). Centrally active following oral administration in vivo.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
化合物库 for SB 206553 hydrochloride
SB 206553 hydrochloride 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 206553 hydrochloride
| 分子量 | 328.8 |
| 公式 | C17H16N4O.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1197334-04-5 |
| PubChem ID | 11957707 |
| InChI Key | VGEMBOFBPSNOIO-UHFFFAOYSA-N |
| Smiles | Cl.CN1C=CC2=CC3=C(CCN3C(=O)NC3=CC=CN=C3)C=C12 |
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 206553 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 32.88 | 100 |
制备储备液 for SB 206553 hydrochloride
以下数据基于产品分子量 328.8。 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 | 3.04 mL | 15.21 mL | 30.41 mL |
| 5 mM | 0.61 mL | 3.04 mL | 6.08 mL |
| 10 mM | 0.3 mL | 1.52 mL | 3.04 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
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产品说明书 for SB 206553 hydrochloride
参考文献 for SB 206553 hydrochloride
参考文献是支持产品生物活性的出版物。
Forbes et al (1995) 5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity and oral activity. J.Med.Chem. 38 2524 PMID: 7629791
Kennett et al (1996) In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties. Br.J.Pharmacol. 117 427 PMID: 8821530
Porras et al (2002) 5-HT2A and 5-HT2C/2B receptor subtypes modulate DA release induced in vivo by amphetamine and mor. in both the rat nucleus accumbens and striatum. Neuropsychopharmacology 26 311 PMID: 11850146
If you know of a relevant reference for SB 206553 hydrochloride, please let us know.
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关键词: SB 206553 hydrochloride, SB 206553 hydrochloride supplier, Potent, selective, 5-HT2C/5-HT2B, antagonists, Serotonin, 5-HT2B, Receptors, 5-HT2C, SB206553, hydrochloride, GlaxoSmithKline, GSK, 1661, Tocris Bioscience
9 篇 SB 206553 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SB 206553 hydrochloride 的部分引用包括：
Fouad et al (2010) Locomotion after spinal cord injury depends on constitutive activity in serotonin receptors. J Neurophysiol 104 2975 PMID: 20861436
Canal et al (2010) The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen. Psychopharmacology (Berl) 209 163 PMID: 20165943
Murray et al (2010) Recovery of motoneuron and locomotor function after spinal cord injury depends on constitutive activity in 5-HT2C receptors. Nat Med 16 694 PMID: 20512126
Li et al (2014) Synthesis, transport, and metabolism of serotonin formed from exogenously applied 5-HTP after spinal cord injury in rats. J Neurophysiol 111 145 PMID: 24068759
Kuo et al (2014) A xanthine-derivative K(+)-channel opener protects against serotonin-induced cardiomyocyte hypertrophy via the modulation of protein kinases. Int J Biol Sci 10 64 PMID: 24391452
Delaney et al (2011) Pulmonary vascular effects of serotonin and selective serotonin reuptake inhibitors in the late-gestation ovine fetus. Am J Physiol Lung Cell Mol Physiol 301 L937 PMID: 21908589
Li et al (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med 23 733 PMID: 28459438
Bigford et al (2012) 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization. J Biol Chem 287 11049 PMID: 22291020
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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Effects of SB-206553 on MDMA-induced changes in dorsal striatal electrophysiology.
By
Kevin Ball on 01/25/2019
分析类型： In Vivo
种属： Rat
We assessed the effect of SB-206553 (2.0 mg/kg, s.c.) on dorsal striatal single-unit electrophysiology following MDMA (ecstasy; 5.0 mg/kg) administration. A coefficient-of-variation analysis indicated significantly less variability in the magnitude of both MDMA-induced neuronal excitations and inhibitions in rats that were pretreated with SB-206553 compared to vehicle (shown in figure).
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.
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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.
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