D1/D5 Receptor agonist-1
D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC50s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a Ki of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits β-arrestin signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease.
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- Formule: C18H13FN4O4
- Masse moléculaire:368.32
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
D1 Receptor |
D5 Receptor |
In Vitro
D1/D5 Receptor agonist-1 (Compound 24) (10-4-10 μM) maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC50s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a Ki of 111 nM (D1R binding affinity)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-OHDA and L-DOPA (HY-N0304)-induced dyskinesias in adult male SD rats (180 g)[1]
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Dosage:0.3, 1, 3 mg/kg
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Administration:p.o. for a single dose
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Result:Decreased EEG beta power over a longer time course (up to 4 h).
Showed comparable efficacy to a therapeutic dose of L-DOPA and with significantly fewer concomitant dyskinesias at doses with predicted D1 RO of 30 to 50%.
Chemical Information
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Masse moléculaire 368.32
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Formule C18H13FN4O4
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SMILES
FC1=C(C2=C(C)C(NC(N2C)=O)=O)N=CC(OC3=C(C=CO4)C4=CC=N3)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
D1/D5 Receptor agonist-1 Related Classifications
HY-175001 Related Classifications
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