SB-200646A

• 常用名: SB-200646A
• 英文名: SB-200646A
• CAS号: 143797-62-0
• 分子量: 302.759
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₅H₁₅ClN₄O
• 熔点: N/A
• 闪点: N/A

SB-200646A用途

SB-200646A 是第一个对 5-HT2B/2C 的选择性超过 5-HT2A 的拮抗剂,5-HT2B,5-HT2C 和 5-HT2A 的 pKi 值分别为 7.5、6.9 和 5.2。SB-200646A 具有口服活性,在体内具有电生理和抗焦虑特性。

SB-200646A名称

• 中文名: SB 200646盐酸盐
• 英文名: N-(1-Methyl-1H-5-indolyl)-N'-(3-pyridinyl)urea hydrochloride

SB-200646A生物活性

• 描述: SB-200646A 是第一个对 5-HT2B/2C 的选择性超过 5-HT2A 的拮抗剂,5-HT2B,5-HT2C 和 5-HT2A 的 pKi 值分别为 7.5、6.9 和 5.2。SB-200646A 具有口服活性,在体内具有电生理和抗焦虑特性。
• 相关类别:
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
• 靶点实验:

  5-HT2B Receptor:7.5 (pKi)

  5-HT2C Receptor:6.9 (pKi)

  5-HT2A Receptor:5.2 (pKi)

• 体外研究: SB200646A(4μM)消除了乙醇引起的微小抑制性突触后电流(mIPSC)频率的增加,对基础mIPSC频率没有影响[1]。
• 体内研究: SB-200646A(20 mg/kg；静脉注射；每天；持续21天；雄性白化Sprague-Dawley大鼠)治疗可显著减少自发性活动腹侧被盖区(VTA)多巴胺能神经元的数量[1]。静脉注射4-16 mg/kg的SB-200646A可显著提高自发活动的VTA多巴胺能神经元的放电率和爆发事件百分比,并显著增加黑质致密部(SNC)多巴胺能神经元的爆发事件百分比[1]。动物模型：雄性白化Sprague-Dawley大鼠(治疗开始时200-225g,实验时300-350g)[1]剂量：20mg/kg给药：静脉注射；每日；持续21天。结果：腹侧被盖区(VTA)多巴胺能神经元的数量显著减少。
• 参考文献:

  [1]. Blackburn TP, et al. The acute and chronic administration of the 5-HT(2B/2C) receptor antagonist SB-200646A significantly alters the activity of spontaneously active midbrain dopamine neurons in the rat: An in vivo extracellular single cell study. Synapse. 2006 Jun 15;59(8):502-12.

  [2]. Kennett GA, et al. In vivo properties of SB 200646A, a 5-HT2C/2B receptor antagonist. Br J Pharmacol. 1994 Mar;111(3):797-802.

  [3]. Theile JW, et al. Role of 5-hydroxytryptamine2C receptors in Ca2+-dependent ethanol potentiation of GABA release onto ventral tegmental area dopamine neurons. J Pharmacol Exp Ther. 2009 May;329(2):625-33.

SB-200646A物理化学性质

• 分子式: C₁₅H₁₅ClN₄O
• 分子量: 302.759
• 精确质量: 302.093445
• InChIKey: IGRYPUQJEDJLHC-UHFFFAOYSA-N
• SMILES: Cl.Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21
• 储存条件: 2-8°C

SB-200646A靶点实验

查看更多实验

实验名称：Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 来源：ChEMBL 靶标：N/A External Id：CHEMBL1266185

实验名称：Antagonistic binding affinity measured against 5-hydroxytryptamine 2A receptor (human... 来源：ChEMBL 靶标：N/A External Id：CHEMBL852624

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：Tocris HTS for Inhibitors of Aerobactin Synthetase lucA 来源：23265 External Id：IucA Pilot Assay Tocris Library

实验名称：LOPAC HTS for Inhibitors of Aerobactin Synthetase IucA 来源：23265 靶标：IucA from hypervirulent Klebsiella pneumoniae External Id：IucA Pilot Assay LOPAC Library

实验名称：Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green ... 来源：ChEMBL 靶标：Plasmodium falciparum External Id：CHEMBL1267249

实验名称：Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green a... 来源：ChEMBL 靶标：Plasmodium falciparum External Id：CHEMBL1267251

实验名称：HTS to identify compounds that affect the blood-brain barrier permeability in vitro 来源：26908 靶标：N/A External Id：HTS97080

实验名称：In vivo potency to block hypolocomotion response to m-CPP in rat after oral administr... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL788095

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify activators of... 来源：The Scripps Research Institute Molecular Screening Center 靶标：N/A External Id：FBW7_ACT_ALPHA_1536_1X%ACT PRUN

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SB-200646A英文别名

• 1-(1-Methyl-1H-indol-5-yl)-3-(3-pyridinyl)urea hydrochloride (1:1)
• Urea, N-(1-methyl-1H-indol-5-yl)-N'-3-pyridinyl-, hydrochloride (1:1)
• 1-(1-Methyl-1H-indol-5-yl)-3-pyridin-3-ylurea hydrochloride (1:1)
• N-(1-Methyl-1H-5-indolyl)-N'-(3-pyridinyl)urea hydrochloride