SB 242084 是一种具有选择性、竞争性和高亲和力的 (pKi=9.0) 的5-HT2C受体拮抗剂 (可透过血脑屏障)。SB 242084 能增加中脑腹侧被盖区 (VTA) 多巴胺能神经元的基础活性和伏隔核中多巴胺的释放。SB 242084 还可通过5-HT2A受体增加线粒体基因的表达和氧化代谢。SB 242084 在焦虑、抑郁和精神分裂症的阴性症状以及急性器官损伤方面具有较好的研究潜力。
| 生物活性 | SB 242084 is a selective, competitive and high-affinity (pKi=9.0)5-HT2Creceptorantagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via5-HT2Areceptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage[1][2][3]. |
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体外研究
(In Vitro) | SB 242084 (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT2Creceptor in SH-SY5Y cells[1].
SB 242084 (1-100 Nm; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC[2].
Cell Viability Assay[1] | Cell Line: | SH-SY5Y cells | | Concentration: | 100 nM | | Incubation Time: | 45 min | | Result: | Antagonized 5-HT induced concentration-related increase in PI hydrolysis. |
RT-PCR[2] | Cell Line: | RPTC cells | | Concentration: | 1-100 nM | | Incubation Time: | 24 h | | Result: | Increased FCCP-uncoupled respiration and PGC-1α mRNA expression. |
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体内研究
(In Vivo) | SB 242084 (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests[1].
SB 242084 (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats[1].
SB 242084 (5, 10 mg/kg; i.p.; single) increases the levels of basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens of rats[3].
SB 242084 (160-640 μg/kg; i.v.; single) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons, and the bursting activity is also enhanced in the same area, in vivo[3].
| Animal Model: | Male Sprague-Dawley (CD) rats[1]. | | Dosage: | 0.1-1 mg/kg | | Administration: | Intraperitoneal injection; single; 20 min pre-test | | Result: | Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box. |
| Animal Model: | Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model)[1]. | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection; single; 20 min pre-test | | Result: | Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation. |
| Animal Model: | Rats[2]. | | Dosage: | 5, 10 mg/kg | | Administration: | Intraperitoneal injection; single | | Result: | Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 44 mg/mL(111.43 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.5326 mL | 12.6630 mL | 25.3261 mL | | 5 mM | 0.5065 mL | 2.5326 mL | 5.0652 mL | | 10 mM | 0.2533 mL | 1.2663 mL | 2.5326 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.33 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.33 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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