SB 242084 monohydrochloride 

SB 242084 monohydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 monohydrochloride 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-HT_2A receptor. SB 242084 monohydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage^[1][2][3].

SB 242084 monohydrochloride (100 nM；45 分钟) 对 SH-SY5Y 细胞中人 5-HT_2C 受体刺激的磷脂酰肌醇水解增加的 5-HT 具有拮抗作用^[1]。
SB 242084 monohydrochloride (1-100 Nm；24 小时) 增加 RPTC 中的 RPTC 呼吸和 PGC-1α mRNA 表达^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SB 242084 monohydrochloride (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^[1]。
SB 242084 monohydrochloride (5 mg/kg；腹腔注射；single；20 min pre-test) 改善 mCPP 诱导的大鼠吞咽不足^[1]。
SB 242084 monohydrochloride (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^[3]。
SB 242084 monohydrochloride (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^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

431.32

C₂₁H₂₀Cl₂N₄O₂

1260505-34-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.  [Content Brief]

  [2]. Harmon JL, et al. 5-HT2 Receptor Regulation of Mitochondrial Genes: Unexpected Pharmacological Effects of Agonists and Antagonists. J Pharmacol Exp Ther. 2016 Apr;357(1):1-9.  [Content Brief]