Sarizotan
CAS No. : 351862-32-3
(Synonyms: EMD 128130)
| Size | Price | Stock |
|---|---|---|
| 5mg | $250 | In-stock |
| 10mg | $380 | In-stock |
| 25mg | $750 | In-stock |
| 50mg | $1200 | In-stock |
| 100mg | $1950 | In-stock |
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| Cat. No. : | HY-100820 |
| M.Wt: | 348.41 |
| Formula: | C22H21FN2O |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
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[1].
In Vitro: Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) [1].
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[1].
Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease[1].
Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats[2].
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