Sarizotan
Based on 1 publication(s) in Google Scholar
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.
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- Pureté: 98.23%
- CAS No.: 351862-32-3
- Formule: C22H21FN2O
- Masse moléculaire:348.41
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Stockage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Sarizotan
MoreVoir tous les produits spécifiques à Isoform 5-HT Receptor
MoreVoir tous les produits spécifiques à Isoform Dopamine Receptor
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Activité biologique
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5-HT1A Receptor 6.5 nM (IC50, rat) |
5-HT1A Receptor |
5-HT1A Receptor 0.1 nM (IC50, human) |
rD2 Receptor 15.1 nM (IC50, rat) |
D3 Receptor 6.8 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) |
hD4.2 Receptor 2.4 nM (IC50) |
hD2 Receptor 17 nM (IC50) |
Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response)[2].
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Dosage:1 ng, 10 ng and 1 μg in 0.3 μL solution.
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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.
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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).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 351862-32-3
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Appearance Viscous Liquid
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Masse moléculaire 348.41
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Formule C22H21FN2O
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Color Colorless to light yellow
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SMILES
FC1=CC=C(C2=CN=CC(CNC[C@H]3CCC4=CC=CC=C4O3)=C2)C=C1
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Synonyms
EMD 128130
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
MAL2 reprograms lipid metabolism in intrahepatic cholangiocarcinoma via EGFR/SREBP-1 pathway based on single-cell RNA sequencing. [Abstract]2024 Jun 12;15(6):411. PMID: 38866777
Solvant et solubilité
DMSO : 100 mg/mL (287.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8702 mL | 14.3509 mL | 28.7018 mL | 71.7545 mL |
| 5 mM | 0.5740 mL | 2.8702 mL | 5.7404 mL | 14.3509 mL | |
| 10 mM | 0.2870 mL | 1.4351 mL | 2.8702 mL | 7.1755 mL | |
| 15 mM | 0.1913 mL | 0.9567 mL | 1.9135 mL | 4.7836 mL | |
| 20 mM | 0.1435 mL | 0.7175 mL | 1.4351 mL | 3.5877 mL | |
| 25 mM | 0.1148 mL | 0.5740 mL | 1.1481 mL | 2.8702 mL | |
| 30 mM | 0.0957 mL | 0.4784 mL | 0.9567 mL | 2.3918 mL | |
| 40 mM | 0.0718 mL | 0.3588 mL | 0.7175 mL | 1.7939 mL | |
| 50 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4351 mL | |
| 60 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1959 mL | |
| 80 mM | 0.0359 mL | 0.1794 mL | 0.3588 mL | 0.8969 mL | |
| 100 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL |
Sarizotan Related Classifications
HY-100820 Related Classifications
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