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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.23%
- CAS 番号: 351862-32-3
- 分子式: C22H21FN2O
- 分子量:348.41
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保管条件:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Sarizotan
More5-HT Receptor アイソフォーム固有の製品をすべて表示
MoreDopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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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 |
化学情報
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CAS 番号 351862-32-3
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性状 Viscous Liquid
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分子量 348.41
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分子式 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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別名
EMD 128130
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (273 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-100820 関連分類
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