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Comedolytic effect of a novel RARgamma-specific retinoid, ER36009: comparison with retinoic acid in the rhino mouse model.

作者信息

Sakuta Tomohiro, Kanayama Toshiji

机构信息

Shiseido Pharmaceutical Research Center 2-12-1 Kanazawa-ku Fukuura, Yokohama, Japan 236-8643.

出版信息

Eur J Dermatol. 2005 Nov-Dec;15(6):459-64.

PMID:16280299
Abstract

In addition to natural retinoids, new synthetic retinoids, such as adapalene and tazarotene, are currently available for the treatment of acne. In this study, we evaluated the comedolytic effect of a novel retinoic acid receptor (RAR)-gamma specific retinoid, ER36009, in the rhino mouse. The animals were treated for five days a week with ER36009 (0.00001, 0.000025, 0.00010, 0.00025%), all-trans-retinoic acid (RA) (0.001, 0.005, 0.010, 0.050%), two commercial formulations (Differine((R)) 0.1% adapalene gel, and Tazorac 0.1% tazarotene gel) and acetone as a control, for two weeks. After the treatments, utricle diameter and apoptosis of the follicular epidermis were examined. ER36009 was 96 times more potent than RA in the utricle diameter reduction assay. It also eliminated apoptosis of the follicular epidermis and restored normal apoptosis at the granular layer. These data indicate that ER36009 is a potent comedolytic agent compared with other currently available retinoids.

摘要

相似文献

1
Comedolytic effect of a novel RARgamma-specific retinoid, ER36009: comparison with retinoic acid in the rhino mouse model.
Eur J Dermatol. 2005 Nov-Dec;15(6):459-64.
2
Marked improvement induced in photoaged skin of hairless mouse by ER36009, a novel RARgamma-specific retinoid, but not by ER35794, an RXR-selective agonist.新型RARγ特异性维甲酸ER36009可使无毛小鼠光老化皮肤有显著改善,但RXR选择性激动剂ER35794则无此效果。
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The Mexican hairless dog as a model for assessing the comedolytic and morphogenic activity of retinoids.墨西哥无毛犬作为评估维甲酸的抗粉刺和形态发生活性的模型。
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The rhino mouse model: the effects of topically applied all-trans retinoic acid and CD271 on the fine structure of the epidermis and utricle wall of pseudocomedones.犀牛鼠模型:局部应用全反式维甲酸和CD271对闭合性粉刺表皮和囊壁精细结构的影响
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引用本文的文献

1
Differential activity of 2-methylene-19-nor vitamin D analogs on growth factor gene expression in rhino mouse skin and comparison to all-trans retinoic acid.2-亚甲基-19-去甲维生素D类似物对犀牛小鼠皮肤生长因子基因表达的差异活性及与全反式维甲酸的比较。
PLoS One. 2017 Nov 28;12(11):e0188887. doi: 10.1371/journal.pone.0188887. eCollection 2017.
2
Topical ER36009, a RARgamma-selective retinoid, decreases abdominal white adipose tissue and elicits changes in expression of genes related to adiposity and thermogenesis.局部应用ER36009,一种视黄酸受体γ选择性类视黄醇,可减少腹部白色脂肪组织,并引起与肥胖和产热相关基因表达的变化。
Endocrine. 2006 Aug;30(1):113-9. doi: 10.1385/ENDO:30:1:113.