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)。

Sarizotan (EMD 128130) is an orally active serotonin 5-HT 1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC 50 values of 6.5 nM (rat 5-HT 1A ), 0.1 nM (human 5-HT 1A ), 15.1 nM (rat D 2 ), 17 nM (human D 2 ), 6.8 nM (human D 3 ) and 2.4 nM (human D 4.2 ), respectively.

Viscous liquid

5-HT1A Receptor 6.5 nM (IC50, rat) 5-HT1A Receptor

Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) . has not independently confirmed the accuracy of these methods. They are for reference only.

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

Room temperature in continental US; may vary elsewhere.

Pure form -20°C 3 years；4°C 2 years

[1]. G D Bartoszyk, et al. Sarizotan, a Serotonin 5-HT1A Receptor Agonist and Dopamine Receptor Ligand. J Neural Transm (Vienna). 2004 Feb;111(2):113-26.
[2]. C Marin, et al. Local Administration of Sarizotan Into the Subthalamic Nucleus Attenuates Levodopa-Induced Dyskinesias in 6-OHDA-lesioned Rats. Psychopharmacology (Berl). 2009 Jun;204(2):241-50.

In Vitro: DMSO : 100 mg/mL (287.02 mM; Need ultrasonic)配制储备液