Ropinirole (Synonyms: SKF 101468)

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Ropinirole (SKF 101468) is an orally active, potent D₃/D₂ receptor agonist with a K_i 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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Ropinirole Chemical Structure

CAS No. : 91374-21-9

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Other In-stock Forms of Ropinirole:

Ropinirole hydrochloride

Other Forms of Ropinirole:

2 Publications Citing Use of MCE Ropinirole

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]^[2]

D₂ Receptor

29 nM (Ki)

hD₂ Receptor

7.4 (pEC₅₀)

hD₃ Receptor

8.4 (pEC₅₀)

hD_4.4 Receptor

6.8 (pEC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
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	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 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]
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	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	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	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	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]

In Vitro

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.

In Vivo

Ropinirole (0.1-10 mg/kg; i.p.) decreases intracranial self-stimulation (ICSS) thresholds and induces anxiolytic- and antidepressive-like effects without affecting motor activity or spatial memory^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

260.37

Formula

C₁₆H₂₄N₂O

CAS No.

91374-21-9

SMILES

O=C1NC2=C(C(CCN(CCC)CCC)=CC=C2)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

Ropinirole Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ropinirole91374-21-9SKF 101468SKF101468SKF-101468Dopamine ReceptorD3D2D1D4Parkinson'sdiseaseInhibitorinhibitorinhibit

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