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(Rac)-Tavapadon

Names

[ CAS No. ]:
1643462-64-9

[ Name ]:
(Rac)-Tavapadon

Biological Activity

[Description]:

(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease

[Target]

D1 Receptor


[In Vitro]

(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751; compound 32) has EMAXs of 118% and 30% in the GS activation assay and the β-arrestin2 recruitment assay[1].

[References]

[1]. Michael L Martini, et al. Designing Functionally Selective Noncatechol Dopamine D 1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity. ACS Chem Neurosci. 2019 Sep 18;10(9):4160-4182.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H16F3N3O3

[ Molecular Weight ]:
391.34

Related Compounds