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Topical betamethasone 17-valerate is an anticorticosteroid in the rat. 1. Dermal atrophy.

作者信息

Young J M, Yoxall B E, Wagner B M

出版信息

Br J Dermatol. 1978 Dec;99(6):655-63. doi: 10.1111/j.1365-2133.1978.tb07060.x.

DOI:10.1111/j.1365-2133.1978.tb07060.x
PMID:737128
Abstract

In the albino rat, topical betamethasone 17-valerate acts as an anticorticosteroid. This steroid is inactive in a dermal atrophy assay over a dose range where betamethasone and hydrocortisone display atrophogenic activity. At appropriate concentrations betamethasone 17-valerate competitively inhibits the atrophogenic effects of both betamethasone and triamcinolone acetonide. Since betamethasone and betamethasone 17-valerate penetrate rat skin in vivo at essentially the same rate, it is concluded that the latter compound is relatively resistant to hydrolysis during penetration, and that it binds to rat corticosteroid receptor proteins in such a manner as to prevent expression of corticosteroid activity. Therefore, the rat cannot be used as a model species to predict activity in man for this compound.

摘要

相似文献

1
Topical betamethasone 17-valerate is an anticorticosteroid in the rat. 1. Dermal atrophy.
Br J Dermatol. 1978 Dec;99(6):655-63. doi: 10.1111/j.1365-2133.1978.tb07060.x.
2
Topical betamethasone 17-valerate is an anticorticosteroid in the rat. 2. Anti-inflammatory and anti-lymphocyte activities.
Br J Dermatol. 1978 Dec;99(6):665-73. doi: 10.1111/j.1365-2133.1978.tb07061.x.
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Steroid atrophy--a histological appraisal.类固醇性萎缩——组织学评估
Dermatologica. 1976;152 Suppl 1:107-15. doi: 10.1159/000257871.
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Onset of the vasoconstrictor effect of diflucortolone valerate, betamethasone valerate, and fluocinolone acetonide ointments applied for varying periods under occlusive dressings.
Dermatologica. 1976;153(4):236-42. doi: 10.1159/000251062.
5
Methods for the assessment of skin atrophogenicity of topical corticosteroids.局部用皮质类固醇皮肤萎缩性评估方法。
Dermatologica. 1976;152 Suppl 1:117-26. doi: 10.1159/000257872.
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BETAMETHASONE 17-VALERATE: A NEW TOPICAL CORTICOSTEROID.倍他米松17-戊酸酯:一种新型外用皮质类固醇。
Lancet. 1964 May 30;1(7344):1177-9. doi: 10.1016/s0140-6736(64)91205-x.
7
Corticosteroid-induced dermal atrophy in the rat.大鼠皮质类固醇诱导的皮肤萎缩
J Invest Dermatol. 1977 Nov;69(5):458-62. doi: 10.1111/1523-1747.ep12511301.
8
Inhibition of acid mucopolysaccharide synthesis by hydrocortisone, hydrocortisone 17-butyrate and betamethasone 17-valerate.
Br J Dermatol. 1977 Nov;97(5):505-7. doi: 10.1111/j.1365-2133.1977.tb14127.x.
9
Pharmacological evaluation of a new topical preparation containing dextran sulphate and betamethasone 17-valerate.一种含有硫酸葡聚糖和倍他米松17-戊酸酯的新型局部用制剂的药理学评价。
Arzneimittelforschung. 1980;30(4):647-51.
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Plasma cortisol levels in normal volunteers receiving either betamethasone valerate or desoximetasone by topical application.正常志愿者局部应用戊酸倍他米松或去氧米松后血浆皮质醇水平。
S Afr Med J. 1978 Aug 5;54(6):239-41.

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