Tavapadon 是一种具有口服活性，高选择性的多巴胺D1/D5受体部分激动剂，它可有效促进运动并减少残疾，对帕金森氏病具有潜在的应用价值。

Tavapadon is an orally active and highly selective dopamine D1/D5 receptor partial agonist.

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. Tavapadon (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. Tavapadon (0.04 mg/kg, s.c.) also improves parkinsonian disability scores with the maximal improvement observed at 110 min after drug administration. Higher doses of Tavapadon (0.1 and 0.15 mg/kg; s.c.) cause statistically significant improvement relative to vehicle in locomotor activity [1].

1643489-24-0

C19H16F3N3O3

391.34

PF-6649751;CVL-751;Tavapadon

DMSO:60 mg/ml (153.32 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years