Pergolide
Based on 1 publication(s) in Google Scholar
Pergolide (LY127809 free base), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptor agonist. Pergolide can be used for Parkinson's disease and hyperprolactinaemia research.
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: 98.59%
- CAS 番号: 66104-22-1
- 分子式: C19H26N2S
- 分子量:314.49
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
MedChemExpress（MCE）の使用を引用している文献 Pergolide
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
製品説明
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D1 Receptor |
D2 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | EC50 |
4.31 nM
Compound: Pergolide
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Agonist activity at Rattus norvegicus (rat) dopamine D2/D3 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
Agonist activity at Rattus norvegicus (rat) dopamine D2/D3 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
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10.1007/s00044-004-0006-x |
| COS-7 | EC50 |
7.86 nM
Compound: Pergolide
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Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
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10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
2.41 nM
Compound: Pergolide
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Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
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10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
27.5 nM
Compound: Pergolide
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Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
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10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
32 nM
Compound: Pergolide
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Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
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10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
5.12 nM
Compound: Pergolide
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Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
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10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
5.59 nM
Compound: Pergolide
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Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
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10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
5.85 nM
Compound: Pergolide
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Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
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10.1007/s00044-004-0006-x |
体外実験
Pergolide (10 nM-50 μM) treatment dose-dependently inhibits H2O2-induced cell death in SH-SY5Y neuroblastoma cells, acting in very low concentrations (nanomolar range) and in very early stages of the neurotoxic intracellular process[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (200-250 g) induced with 6-hydroxydopamine (6-OHDA)[3]
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Dosage:0.3 mg/kg
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Administration:Intraperitoneal injection; daily; 11 days
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Result:A reduced number of working/reference memory errors was observed. And significant decreased of MDA level.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 66104-22-1
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性状 Solid
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分子量 314.49
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分子式 C19H26N2S
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Color White to off-white
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SMILES
[H][C@@]1(N(CCC)C[C@H](CSC)C[C@@]12[H])CC3=CNC4=CC=CC2=C43
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別名
LY127809 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -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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Nature
2023 Dec;624(7992):672-681. PMID: 37935376
溶剤 & 溶解度
体外:
DMSO : 4.17 mg/mL (13.26 mM; ultrasonic and warming and heat to 60°C; 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 (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. S Franks, et al. Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia. Br Med J (Clin Res Ed). 1983 Apr 9;286(6372):1177-9. [Content Brief]
[2]. Daniela Uberti, et al. Pergolide protects SH-SY5Y cells against neurodegeneration induced by H(2)O(2). Eur J Pharmacol. 2002 Jan 2;434(1-2):17-20. [Content Brief]
[3]. Alin Ciobica, et al. The effects of pergolide on memory and oxidative stress in a rat model of Parkinson's disease. J Physiol Biochem. 2012 Mar;68(1):59-69. [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 | 3.1798 mL | 15.8988 mL | 31.7975 mL | 79.4938 mL |
| 5 mM | 0.6360 mL | 3.1798 mL | 6.3595 mL | 15.8988 mL | |
| 10 mM | 0.3180 mL | 1.5899 mL | 3.1798 mL | 7.9494 mL |
Pergolide 関連分類
HY-13720 関連分類
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Keywords
- Pergolide
- 66104-22-1
- LY127809
- LY 127809
- LY-127809
- Dopamine Receptor
- Drug Derivative
- hyperprolactinemia-related diseases
- postsynaptic central dopaminergic receptors
- dopamine receptor agonist
- X-ray crystallography
- restrictive valvular heart disease
- heart valve leaflets
- serotonin 5-HT2B receptor
- Parkinson's disease
- pulmonary hypertension
- restless legs syndrome
- Inhibitor
- inhibitor
- inhibit