Sarizotan,351862-32-3

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Sarizotan

CAS No. : 351862-32-3

MCE 国际站：Sarizotan

产品活性：Sarizotan (EMD 128130) 是具有口服活性的 5-HT_1A 受体 和多巴胺受体的激动剂，其 IC₅₀ 值分别为 6.5 nM (rat 5-HT_1A)、 0.1 nM (human 5-HT_1A)、15.1 nM (rat D₂)、17 nM (human D₂)、6.8 nM (human D₃) 和 2.4 nM (human D_4.2)。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor  |  Dopamine Receptor

In Vitro: Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC₅₀ value of 150 nM (E_max 40% at 1 mM) .

In Vivo: 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.

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