Department of Chemistry, Michigan Laboratories, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105, United States.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):306-8. doi: 10.1016/j.bmcl.2009.10.109. Epub 2009 Oct 29.
A thyroid hormone receptor beta subtype-selective thyromimetic 5 was found to be efficacious in both mouse and monkey hair growth models after topical applications. It penetrates the skin according to the test in human cadaver skin mounted onto Franz diffusion chambers. The serum drug level of 5 is below the limit of quantification during tests in the bald stump-tailed macaques (Macaca arctoides). It is tested negative in the 3T3 neutral red uptake (NRU) phototoxicity test, indicating a low risk for causing photo-irritation. It is also rapidly metabolized according to the PK data, thus the systemic exposure is limited.
一种甲状腺激素受体β亚型选择性甲状腺刺激物 5 在经过局部应用后，在小鼠和猴的毛发生长模型中均显示出疗效。根据在 Franz 扩散室中安装的人体尸体皮肤进行的测试，它可以穿透皮肤。在无毛短尾猕猴（Macaca arctoides）的测试中，5 的血清药物水平低于定量限。它在 3T3 中性红摄取（NRU）光毒性测试中呈阴性，表明引起光刺激性的风险较低。根据 PK 数据，它也被迅速代谢，因此全身暴露有限。
