|(-)-1,5-二甲基-6-(2-甲基-4-((3-(三氟甲基)吡啶-2-基)氧基)苯基)嘧啶-2,4(1H,3H)-二酮|CsnPharm

CAS No.: 1643489-24-0

Tavapadon Catalog No. CSN28443

Synonyms: PF-06649751;CVL-751;PF-6649751

Tavapadon is an orally active and highly selective dopamine D1/D5 receptor partial agonist. It may be useful in the treatment of Parkinson's disease and Alzheimer's.

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生物活性

描述Tavapadon is an orally active and highly selective dopamine D1/D5 receptor partial agonist. It may be useful in the treatment of Parkinson's disease and Alzheimer's. 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]. The most frequently reported adverse events in patients treated with tavapadon were nausea, headache, dry mouth, somnolence, and tremor^[2].
参考文献

[1] Young D, Popiolek M, Trapa P, Fonseca KR, Brevard J, Gray DL, Kozak R. D1 Agonist Improved Movement of Parkinsonian Nonhuman Primates with Limited Dyskinesia Side Effects. ACS Chem Neurosci. 2020 Feb 19;11(4):560-566.
[2] Cerevel Therapeutics Announces Positive Results from a Phase 2 Study of Tavapadon in Patients with Early-stage Parkinson’s Disease.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5553 mL
- 12.7765 mL
- 25.5530 mL
- 5 mM
- 0.5111 mL
- 2.5553 mL
- 5.1106 mL
- 10 mM
- 0.2555 mL
- 1.2776 mL
- 2.5553 mL

技术信息

CAS号	1643489-24-0	储存条件	粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C19H16F3N3O3	运输	蓝冰
分子量	391.34	别名	PF-06649751;CVL-751;PF-6649751

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