Bioactivity | (Rac)-Tavapadon ((Rac)-PF-06649751) 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]. | ||||||||||||
Invitro | (Rac)-Tavapadon ((Rac)-PF-06649751; compound 32) has EMAXs of 118% and 30% in the GS activation assay and the β-arrestin2 recruitment assay[1]. | ||||||||||||
Name | (Rac)-Tavapadon | ||||||||||||
CAS | 1643462-64-9 | ||||||||||||
Formula | C19H16F3N3O3 | ||||||||||||
Molar Mass | 391.34 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |