Tavapadon

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tavapadon (PF 6649751, PF-06649751) 是一种口服多巴胺 D1 受体部分激动剂，用于治疗帕金森病。

Tavapadon (PF 6649751, PF-06649751) is an orally available dopamine D1 receptor partial agonist for treatment of Parkinson's disease.Parkinson Disease Discontinued.

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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. 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.) leads to statistically significant improvement relative to vehicle in locomotor activity. 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.

PF 6649751 | PF-06649751

GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

Neurological Disease

Parkinson Disease

1643489-24-0

391.35

C19H16F3N3O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (255.53 mM)

O=C1NC(C(C)=C(C2=CC=C(OC3=NC=CC=C3C(F)(F)F)C=C2C)N1C)=O

(-)-1,5-Dimethyl-6-[2-methyl-4-[[3-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]-2,4(1H,3H)-pyrimidinedione

(-20℃)

With Ice Pack

≥ 2 years