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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[1].

Product Specifications

UNSPSC

12352005

Target

Arrestin; Dopamine Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Smiles

FC1=C(C2=C(C)C(NC(N2C)=O)=O)N=CC(OC3=C(C=CO4)C4=CC=N3)=C1

Molecular Formula

C18H13FN4O4

Molecular Weight

368.32

References & Citations

[1]Rodríguez Sarmiento RM, et al. Orally Bioavailable Dopamine D1/D5 Receptor-Biased Agonists to Study the Role of β-Arrestin in Treatment-Related Dyskinesia in Parkinson's Disease. J Med Chem. 2025 Jul 10;68 (13) :13532-13561.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

D1 Receptor; D5 Receptor

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