SB 206553 hydrochloride

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Cat.No. 1661 - SB 206553 hydrochloride | C17H16N4O.HCl | CAS No. 1197334-04-5
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)
引用文献 (9)
评论 (1)
文献 (4)

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.


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
Smiles Cl.CN1C=CC2=CC3=C(CCN3C(=O)NC3=CC=CN=C3)C=C12


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
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


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.


查看全部 5-HT2C Receptor Antagonists

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:

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

Li et al (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med 23 733 PMID: 28459438

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

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).

PMID: 16001122 参考文献
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