Bioactivity | 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]. |
Target | dopamine D1/D5 receptor |
In Vivo | 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]. |
Name | Tavapadon |
CAS | 1643489-24-0 |
Formula | C19H16F3N3O3 |
Molar Mass | 391.34 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. |