产品
编 号：F225974
分子式：C21H19ClN4O2
分子量：394.85
分子式：C21H19ClN4O2
分子量：394.85
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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50mg
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结构图
CAS No: 181632-25-7
产品详情
生物活性：
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (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 via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.
体内研究：
SB 242084 (0.1-1 mg/kg；腹腔注射；单次；预测试 20 分钟) 改善大鼠在社交互动测试中的行为。SB 242084 (5 mg/kg；腹腔注射；single；20 min pre-test) 改善 mCPP 诱导的大鼠吞咽不足。SB 242084 (5，10 mg/kg；腹腔注射；single) 增加大鼠伏隔核中基础透析液多巴胺 (DA) 和二羟基苯乙酸 (DOPAC) 的水平。SB 242084 (160-640 μg/kg；静脉注射；单次) 剂量-依赖性显著增加 VTA (腹侧被盖区) 多巴胺能神经元的基础放电率，并且体内同一区域的爆发活动也增强。Animal Model:Male Sprague-Dawley (CD) rats.
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).
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.
Dosage:5, 10 mg/kg
Administration:Intraperitoneal injection; single
Result:Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.
体外研究：
SB 242084 (100 nM；45 分钟) 对 SH-SY5Y 细胞中人 5-HT2C 受体刺激的磷脂酰肌醇水解增加的 5-HT 具有拮抗作用。 SB 242084 (1-100 Nm；24 小时) 增加 RPTC 中的 RPTC 呼吸和 PGC-1α mRNA 表达。
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (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 via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.
体内研究：
SB 242084 (0.1-1 mg/kg；腹腔注射；单次；预测试 20 分钟) 改善大鼠在社交互动测试中的行为。SB 242084 (5 mg/kg；腹腔注射；single；20 min pre-test) 改善 mCPP 诱导的大鼠吞咽不足。SB 242084 (5，10 mg/kg；腹腔注射；single) 增加大鼠伏隔核中基础透析液多巴胺 (DA) 和二羟基苯乙酸 (DOPAC) 的水平。SB 242084 (160-640 μg/kg；静脉注射；单次) 剂量-依赖性显著增加 VTA (腹侧被盖区) 多巴胺能神经元的基础放电率，并且体内同一区域的爆发活动也增强。Animal Model:Male Sprague-Dawley (CD) rats.
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).
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.
Dosage:5, 10 mg/kg
Administration:Intraperitoneal injection; single
Result:Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.
体外研究：
SB 242084 (100 nM；45 分钟) 对 SH-SY5Y 细胞中人 5-HT2C 受体刺激的磷脂酰肌醇水解增加的 5-HT 具有拮抗作用。 SB 242084 (1-100 Nm；24 小时) 增加 RPTC 中的 RPTC 呼吸和 PGC-1α mRNA 表达。
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