产品
编 号：F627386
分子式：C22H30N4O3
分子量：398.5
分子式：C22H30N4O3
分子量：398.5
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
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询价
结构图
CAS No: 1152747-82-4
产品详情
生物活性：
Enerisant (TS-091) is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.
体内研究：
Enerisant hydrochloride (0.3-1 mg/kg; p.o.; once) 减弱大鼠的双食性反应。Enerisant hydrochloride (0.1-3 mg/kg; p.o.; once) 导致大鼠组胺 H3 受体以剂量依赖的方式被占用。引起半最大受体占用的剂量为 0.78 mg/kg。Enerisant hydrochloride (1 mg/kg; s.c.; once) 增加大鼠下丘脑后部的总细胞外组胺水平。Enerisant hydrochloride (1 mg/kg; i.p.; once) 增加大鼠内侧前额叶皮层 (mPFC) 的总细胞外多巴胺和乙酰胆碱水平。Animal Model:Male SD rats, R-α-methylhistamine-induced dipsogenia model
Dosage:0.1, 0.3 and 1 mg/kg
Administration:Oral, single dose
Result:Attenuated the dipsogenia response, reaching statistical significance at doses of 0.3 mg/kg and 1 mg/kg.
Enerisant (TS-091) is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.
体内研究：
Enerisant hydrochloride (0.3-1 mg/kg; p.o.; once) 减弱大鼠的双食性反应。Enerisant hydrochloride (0.1-3 mg/kg; p.o.; once) 导致大鼠组胺 H3 受体以剂量依赖的方式被占用。引起半最大受体占用的剂量为 0.78 mg/kg。Enerisant hydrochloride (1 mg/kg; s.c.; once) 增加大鼠下丘脑后部的总细胞外组胺水平。Enerisant hydrochloride (1 mg/kg; i.p.; once) 增加大鼠内侧前额叶皮层 (mPFC) 的总细胞外多巴胺和乙酰胆碱水平。Animal Model:Male SD rats, R-α-methylhistamine-induced dipsogenia model
Dosage:0.1, 0.3 and 1 mg/kg
Administration:Oral, single dose
Result:Attenuated the dipsogenia response, reaching statistical significance at doses of 0.3 mg/kg and 1 mg/kg.
产品资料
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