Tavapadon

• CAT Number: I016659
• CAS Number: 1643489-24-0
• Molecular Formula: C₁₉H₁₆F₃N₃O₃
• Molecular Weight: 391.34
• Purity: ≥95%
• Target: Neuronal Signaling

Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson’s disease[1].Tavapadon (PF-06649751; 0.02 and 0.04 mg/kg; s.c.) at the 0.04 mg/kg test dose increases locomotor activity, whereas the 0.02 mg/kg dose has little or no effect[1].
Tavapadon (0.04 mg/kg, s.c.) also improves parkinsonian disability scores with the maximal improvement observed at 110 min after drug administration[1].
Higher doses of Tavapadon (0.1 and 0.15 mg/kg; s.c.) leads to statistically significant improvement relative to vehicle in locomotor activity[1].
Tavapadon (0.1 mg/kg; s.c.) has the mean maximal unbound plasma concentration of 8 nM and achieves 3 hours after compound administration in captive-bred macaques[1].

Reference

[1]. Young D, et al. D1 Agonist Improved Movement of Parkinsonian Nonhuman Primates with Limited DyskinesiaSide Effects. ACS Chem Neurosci. 2020 Feb 19;11(4):560-566.