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苯肾上腺素新戊酸酯是前体药物吗?

Is phenylephrine pivalate a prodrug?

作者信息

Mindel J S, Shaikewitz S T, Podos S M

出版信息

Arch Ophthalmol. 1980 Dec;98(12):2220-3. doi: 10.1001/archopht.1980.01020041072016.

Abstract

Phenylephrine pivalate has been assumed to be a prodrug devoid of important intrinsic activity because of its structural similarity to dipivefrin (dipivaly epinephrine). However, unlike dipivefrin, the pharmacologic activity of phenylephrine pivalate was not prevented by prior administration of echothiophate iodide. Rabbits pretreated bilaterally with 0.25% echothiophate for two and seven days had similar mydriasis, both in quantity and duration, after receiving 10% phenylephrine hydrochloride to one eye and 1% phenylephrine pivalate to the other eye. This as consistent with the hypothesis that the phenylephrine pivalate molecule has important alpha-adrenergic activity regardless of whether it is converted to phenylephrine.

摘要

由于去氧肾上腺素新戊酸酯与双特戊酰肾上腺素结构相似,人们一直认为它是一种没有重要内在活性的前药。然而,与双特戊酰肾上腺素不同,预先给予碘依可酯并不会阻止去氧肾上腺素新戊酸酯的药理活性。用0.25%碘依可酯双侧预处理两天和七天的兔子,在一只眼睛滴入10%盐酸去氧肾上腺素,另一只眼睛滴入1%去氧肾上腺素新戊酸酯后,出现了数量和持续时间相似的散瞳现象。这与去氧肾上腺素新戊酸酯分子无论是否转化为去氧肾上腺素都具有重要的α-肾上腺素能活性这一假设相一致。

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