1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor
  3. Sarizotan

Sarizotan (Synonyms: EMD 128130)

Cat. No.: HY-100820
Handling Instructions

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.

For research use only. We do not sell to patients.

Sarizotan Chemical Structure

Sarizotan Chemical Structure

CAS No. : 351862-32-3

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Description

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].

IC50 & Target[1]

5-HT1A Receptor

6.5 nM (IC50, rat)

5-HT1A Receptor

0.1 nM (IC50, human)

D2 Receptor

15.1 nM (IC50, rat)

D2 Receptor

17 nM (IC50, human)

D3 Receptor

6.8 nM (IC50, human)

D4.2

2.4 nM (IC50, human)

5-HT1B Receptor

600 nM (IC50, rat)

5-HT1D Receptor

500 nM (IC50, calf)

5-HT2A Receptor

960 nM (IC50, rat, agonist site)

5-HT2A Receptor

587 nM (IC50, human, antagonist site)

5-HT2B Receptor

108 nM (IC50, human)

5-HT2C Receptor

800 nM (IC50, pig)

5-HT3 Receptor

3500 nM (IC50, NG 108 cells)

5-HT5A Receptor

313 nM (IC50, human)

5-HT6 Receptor

3300 nM (IC50, human)

5-HT7 Receptor

10 nM (IC50, human)

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].

Animal Model: Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response)[2].
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).
Molecular Weight

348.41

Formula

C₂₂H₂₁FN₂O

CAS No.

351862-32-3

SMILES

FC1=CC=C(C2=CN=CC(CNC[[email protected]]3CCC4=CC=CC=C4O3)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SarizotanEMD 128130EMD128130EMD-1281305-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorParkinson’sdiseaseDOPAdyskinesiaInhibitorinhibitorinhibit

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