Ropinirole
Based on 4 publication(s) in Google Scholar
Ropinirole (SKF 101468) is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole has no affinity for the D1 receptors. Ropinirole has the potential for Parkinson's disease.
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- Pureté: 99.42%
- CAS No.: 91374-21-9
- Formule: C16H24N2O
- Masse moléculaire:260.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Ropinirole
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Activité biologique
|
D2 Receptor 29 nM (Ki) |
hD2 Receptor 7.4 (pEC50) |
hD3 Receptor 8.4 (pEC50) |
hD4.4 Receptor 6.8 (pEC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| AtT20 | EC50 |
19.2 nM
Compound: ropinirole
|
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
|
[PMID: 20038106] |
| CHO | EC50 |
10.3 nM
Compound: ropinirole
|
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
[PMID: 20146482] |
| CHO | EC50 |
10.3 nM
Compound: Ropinirole
|
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
[PMID: 20605099] |
| CHO | EC50 |
304 nM
Compound: ropinirole
|
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
[PMID: 20146482] |
| CHO | EC50 |
304 nM
Compound: Ropinirole
|
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
|
[PMID: 25490054] |
| CHO | EC50 |
304 nM
Compound: ropinirole
|
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
|
[PMID: 20038106] |
| CHO | EC50 |
304 nM
Compound: Ropinirole
|
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
[PMID: 20605099] |
| CHO | EC50 |
4 nM
Compound: ropinerole
|
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
|
[PMID: 17976986] |
| COS-7 | EC50 |
3.89 nM
Compound: Ropinirole
|
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
|
10.1007/s00044-004-0006-x |
| COS-7 | EC50 |
75.5 nM
Compound: Ropinirole
|
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
|
10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
107 nM
Compound: Ropinirole
|
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
|
10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
1803 nM
Compound: Ropinirole
|
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
|
10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
56.1 nM
Compound: Ropinirole
|
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
|
10.1007/s00044-004-0006-x |
| COS-7 | IC50 |
985 nM
Compound: Ropinirole
|
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
|
10.1007/s00044-004-0006-x |
| HEK293 | EC50 |
330 nM
Compound: 2
|
Agonist activity at human D2SR expressed in HEK293 cell membranes co-expressing PTX insensitive variant of Galphao1 incubated for 30 mins by [35S]GTP-gammaS binding assay
Agonist activity at human D2SR expressed in HEK293 cell membranes co-expressing PTX insensitive variant of Galphao1 incubated for 30 mins by [35S]GTP-gammaS binding assay
|
[PMID: 28870802] |
| HEK293 | EC50 |
89 nM
Compound: 2
|
Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay
Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay
|
[PMID: 28870802] |
| HEK-293T | EC50 |
30 nM
Compound: Ropinirole
|
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
|
[PMID: 28489379] |
| HEK-293T | EC50 |
330 nM
Compound: Ropinirole
|
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding
|
[PMID: 28489379] |
| HEK-293T | EC50 |
89 nM
Compound: Ropinirole
|
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
|
[PMID: 28489379] |
| Pituitary gland cell | EC50 |
83 nM
Compound: ropinerole
|
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
|
[PMID: 17976986] |
Ropinirole has affinity for D3 receptors of 10-20 fold higher than the D2 and D4 receptors. Ropinirole is weakly active at alpha 2-adrenoceptors and 5-HT2 receptors but inactive at 5-HT1, benzodiazepine and gamma-aminobutyric acid receptors or alpha 1 and beta-adrenoceptors[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 91374-21-9
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Appearance Solid
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Masse moléculaire 260.37
-
Formule C16H24N2O
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Color Pale purple to light pink
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SMILES
O=C1NC2=C(C(CCN(CCC)CCC)=CC=C2)C1
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Synonyms
SKF 101468
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Nigra-Subthalamic Dopaminergic Circuitry Modulates and Represents Distinct Pain Modality in Physiological and Pain States in Mice. [Abstract]2026 Jul;13(37):e19913. PMID: 41944312 -
Acta Pharmacol Sin
Dysfunction of subthalamic dopaminergic circuitry contributes to anxiety- and depression-like behaviors in 6-OHDA lesion-induced hemiparkinsonian mice. [Abstract]2025 May 6. PMID: 40329003 -
Front Cell Dev Biol
Chlorpromazine affects autophagy in association with altered Rag GTPase-mTORC1-TFEB signaling. [Abstract]2023 Sep 8:11:1266198. PMID: 37745295 -
J Neurosci
Acute Ongoing Nociception Delays Recovery of Consciousness from Sevoflurane Anesthesia via a Midbrain Circuit. [Abstract]2024 Aug 21;44(34):e0740242024. PMID: 39019613
Solvant et solubilité
DMSO : 50 mg/mL (192.03 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 (272 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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Instruction de manipulation (2659 KB)
Références
[1]. Eden, R.J., et al., Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist. Pharmacol Biochem Behav, 1991. 38(1): p. 147-54. [Content Brief]
[2]. Mavrikaki M, et al. Ropinirole regulates emotionality and neuronal activity markers in the limbic forebrain. Int J Neuropsychopharmacol. 2014 Dec;17(12):1981-93. [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 | 3.8407 mL | 19.2034 mL | 38.4069 mL | 96.0172 mL |
| 5 mM | 0.7681 mL | 3.8407 mL | 7.6814 mL | 19.2034 mL | |
| 10 mM | 0.3841 mL | 1.9203 mL | 3.8407 mL | 9.6017 mL | |
| 15 mM | 0.2560 mL | 1.2802 mL | 2.5605 mL | 6.4011 mL | |
| 20 mM | 0.1920 mL | 0.9602 mL | 1.9203 mL | 4.8009 mL | |
| 25 mM | 0.1536 mL | 0.7681 mL | 1.5363 mL | 3.8407 mL | |
| 30 mM | 0.1280 mL | 0.6401 mL | 1.2802 mL | 3.2006 mL | |
| 40 mM | 0.0960 mL | 0.4801 mL | 0.9602 mL | 2.4004 mL | |
| 50 mM | 0.0768 mL | 0.3841 mL | 0.7681 mL | 1.9203 mL | |
| 60 mM | 0.0640 mL | 0.3201 mL | 0.6401 mL | 1.6003 mL | |
| 80 mM | 0.0480 mL | 0.2400 mL | 0.4801 mL | 1.2002 mL | |
| 100 mM | 0.0384 mL | 0.1920 mL | 0.3841 mL | 0.9602 mL |