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TitleOrally Bioavailable Dopamine D1/D5 Receptor-Biased Agonists to Study the Role of β-Arrestin in Treatment-Related Dyskinesia in Parkinson's Disease.
Journal, issue, pagesJ Med Chem, Vol. 68, Issue 13, Page 13532-13561, Year 2025
Publish dateJul 10, 2025
AuthorsRosa María Rodríguez Sarmiento / Stefan Berchtold / Nenad Manevski / Lothar Lindemann / Fabian Dey / Thomas Clairfeuille / Davide Amendola / Nicolas Vautrelle / Venceslas Duveau / Eoin C O Connor /
PubMed AbstractDopamine replacement therapies for Parkinson's disease often produce dyskinesias with long-term use. Published studies suggest that introducing β-arrestin signaling might be protective for ...Dopamine replacement therapies for Parkinson's disease often produce dyskinesias with long-term use. Published studies suggest that introducing β-arrestin signaling might be protective for dyskinesia. We advanced known noncatecholamine D1/D5 receptor G protein-biased agonists and found that removal of oxygen in the linker from published compounds limited β-arrestin recruitment, whereas introduction of nitrogen on the central -phenyl linker favored β-arrestin recruitment and provided orally bioavailable compounds. Cryogenic electron microscopy suggested key receptor-ligand interactions influencing the different bias behaviors. We discovered compound , a D1/D5 receptor agonist with β-arrestin recruitment and properties for use . We compared with tavapadon, which shows weak efficacy for β-arrestin signaling, in a rat model of Parkinson's disease with L-DOPA-induced dyskinesias. At particular doses, compound produced efficacy comparable to L-DOPA, but with fewer concomitant dyskinesias. This first study suggests that β-arrestin may have a positive influence on reducing dyskinesias following acute administration.
External linksJ Med Chem / PubMed:40552668
MethodsEM (single particle)
Resolution2.72 - 2.8 Å
Structure data

52624

9i52

EMDB-52624, PDB-9i52:
Dopamine 1 receptor:GaS complex bound to 19B
Method: EM (single particle) / Resolution: 2.8 Å

52625

9i54

EMDB-52625, PDB-9i54:
Dopamine 1 receptor:GaS complex bound to 24
Method: EM (single particle) / Resolution: 2.72 Å

Chemicals


PDB Unreleased entry

PDB-1izu: M30L/F46L mutant of bovine pancreatic ribonuclease A

ChemComp-HOH:
WATER


PDB Unreleased entry

PDB-1izv: M30L/F46V mutant of bovine pancreatic ribonuclease A

Source
  • homo sapiens (human)
KeywordsHORMONE / D1R / GS / AGONIST / PARKINSON / NEUROSCIENCE / D1R GS

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