PW0464

Names

[ Name ]:
PW0464

Biological Activity

[Description]:

PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[In Vitro]

PW0464 (compound 24) is found to elicit complete G protein bias, showing no activity for D1R-mediated β-arrestin recruitment[1]. PW0464 (compound 24), the non-catechol agonist, forms bonds with S1985.42 and S2025.46 via its fluorine atom[2].

[References]

[1]. Pingyuan Wang, et al. Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. ACS Med Chem Lett

[2]. David R Sibley, et al. Novel Cryo-EM structures of the D1 dopamine receptor unlock its therapeutic potential. Signal Transduct Target Ther. 2021 May 22;6(1):205.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₇F₂N₃O₄

[ Molecular Weight ]:
389.35

Related Compounds

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