产品
编 号：F332407
分子式：C22H21FN2O
分子量：348.41
分子式：C22H21FN2O
分子量：348.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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结构图
CAS No: 351862-32-3
产品详情
生物活性：
Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
体内研究：
Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex.Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease.Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats.Animal Model:Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response).
Dosage:1 ng, 10 ng and 1 μg in 0.3 μL solution.
Administration:Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days.
Result:On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively).
体外研究：
Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) .
Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
体内研究：
Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex.Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease.Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats.Animal Model:Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response).
Dosage:1 ng, 10 ng and 1 μg in 0.3 μL solution.
Administration:Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days.
Result:On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively).
体外研究：
Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) .
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