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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.59%
- No. CAS: 66104-22-1
- Fòrmula: C19H26N2S
- Peso molecular:314.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Pergolide
MoreVer todos los productos específicos de isoformas Dopamine Receptor
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Actividad biológica
Descripciòn
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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 |
In Vitro
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.
In Vivo
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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 66104-22-1
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Appearance Solid
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Peso molecular 314.49
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Fòrmula 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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Synonyms
LY127809 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Solvente y solubilidad
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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 Related Classifications
HY-13720 Related Classifications
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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