Michel S, Jomard A, Démarchez M
Galderma R & D, Valbonne, France.
Br J Dermatol. 1998 Oct;139 Suppl 52:3-7. doi: 10.1046/j.1365-2133.1998.1390s2003.x.
Adapalene, a synthetic retinoid, is a new drug proposed for the treatment of acne patients. Studies on the in vitro and in vivo pharmacology of adapalene have shown that it is very active on cell and tissue proliferation and differentiation. Furthermore, adapalene has anti-inflammatory potential as determined by its anti-AP1 activity. Adapalene interacts selectively with the nuclear receptors RAR beta and RAR gamma, and its activity on proliferation and differentiation can be blocked by a RAR beta-gamma antagonist. Because RAR beta is not expressed in human keratinocytes, the effect of adapalene on the major cell type of the epidermis is certainly mediated by its interaction with RAR gamma. The unique pharmacological properties of adapalene may explain why, when compared to tretinoin, it has an improved therapeutic ratio due to its better tolerance.
阿达帕林是一种合成类视黄醇，是一种被提议用于治疗痤疮患者的新药。对阿达帕林的体外和体内药理学研究表明，它在细胞和组织增殖及分化方面具有很高的活性。此外，通过其抗AP1活性测定，阿达帕林具有抗炎潜力。阿达帕林与核受体RARβ和RARγ选择性相互作用，其对增殖和分化的活性可被RARβ-γ拮抗剂阻断。由于RARβ在人类角质形成细胞中不表达，阿达帕林对表皮主要细胞类型的作用肯定是通过其与RARγ的相互作用介导的。阿达帕林独特的药理特性可能解释了为什么与维甲酸相比，它因耐受性更好而具有更高的治疗指数。
