Matias J R, Gaillard M
Nova Biosciences, Norrie Point Research Station, Staatsburg, New York 12553, USA.
Ann N Y Acad Sci. 1995 Jun 12;761:56-65. doi: 10.1111/j.1749-6632.1995.tb31369.x.
The biological activity of a series of nonsteroidal, pure androgen receptor inhibitors was compared using the Syrian hamster ear skin sebaceous gland model. RU 58841, RU 56187, RU 38882 and cyproterone acetate were applied topically for 4 weeks on the ventral ear pinna of sexually mature male Syrian hamsters. Their order of efficacy was as follows: RU 58841 > RU 56187 > RU 38882 > cyproterone acetate. Maximal reduction of 60% in the size of the sebaceous glands was observed in hamsters treated with RU 58841 at a dose of 10 micrograms per day. This degree of inhibition occurred without any systemic side effects as shown by the absence of inhibition on the contralateral untreated ear pinna. Longer treatment did not produce greater inhibition since extending the treatment period from 4 weeks to 12 weeks showed similar data. The effect of RU 58841 was reversible since the inhibited sebaceous glands returned to normal size within 4 weeks after the cessation of the topical applications. The potent localized inhibition of sebaceous glands by RU 58841 demonstrates the excellent potential of this compound as a topical drug for the treatment of acne and other androgen-mediated disorders.
使用叙利亚仓鼠耳皮肤皮脂腺模型比较了一系列非甾体类纯雄激素受体抑制剂的生物活性。将RU 58841、RU 56187、RU 38882和醋酸环丙孕酮局部应用于性成熟雄性叙利亚仓鼠的腹侧耳廓4周。它们的疗效顺序如下：RU 58841 > RU 56187 > RU 38882 > 醋酸环丙孕酮。在用每天10微克剂量的RU 58841治疗的仓鼠中，观察到皮脂腺大小最大减少60%。对侧未治疗的耳廓无抑制作用，表明这种程度的抑制没有任何全身副作用。延长治疗时间并未产生更大的抑制作用，因为将治疗期从4周延长至12周显示了相似的数据。RU 58841的作用是可逆的，因为在局部应用停止后4周内，受抑制的皮脂腺恢复到正常大小。RU 58841对皮脂腺的有效局部抑制作用证明了该化合物作为治疗痤疮和其他雄激素介导疾病的局部用药具有极好的潜力。
