Isotretinoin 是一种天然存在的维甲酸,具有潜在的抗肿瘤活性。 它结合并激活核视黄酸受体 (RAR), 活化的 RARs 作为促进细胞分化和凋亡的转录因子。它是一种类维生素A和维生素A衍生物,用于治疗严重的痤疮和某些形式的皮肤、头颈癌。
半岛bd体育手机客户端 描述
Isotretinoin binds to and activates nuclear retinoic acid receptors (RARs); activated RARs serve as transcription factors that promote cell differentiation and apoptosis. Isotretinoin is a naturally-occurring retinoic acid with potential antineoplastic activity. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.
体外活性
Isotretinoin directly interferes with the development of cranial neural crest cells. [1] Isotretinoin selectively affects neural crest cells by decreasing their cell-substratum adhesion. [2]
体内活性
Isotretinoin (500 ng/mL) and its main metabolite in the human, 4-oxo-isotretinoin, induce malformations similar to those seen in vivo. [1] Isotretinoin impairs explicit memory in Stage 2, but retention tests one month after Isotretinoin exposure ended, indicated recovery from this explicit memory impairment and evidence of enhanced implicit memory in the 10 mg and 15 mg ISO rats. [3] Isotretinoin slows the recovery of rod signaling after exposure to an intense bleaching light, and that rhodopsin regeneration is markedly slowed. Isotretinoin is also found to protect rat photoreceptors from light-induced damage. [4] Isotretinoin blocks the formation of A2E biochemically and the accumulation of lipofuscin pigments by electron microscopy. Isotretinoin also blocks the slower, age-dependent accumulation of lipofuscin in wild-type mice. [5]
Cas No.
4759-48-2
分子式
C20H28O2
分子量
300.442
别名
13-cis-Retinoic acid;异维A酸
储存和溶解度
DMSO:60 mg/mL (199.7 mM)
Ethanol:1 mg/mL (3.32 mM),warmed
Powder: -20°C for 3 years
In solvent: -80°C for 2 years