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前列腺素的作用以及比马前列素在治疗眼压升高和高眼压症中的特定治疗地位:深入探讨比马前列素和前列腺酰胺的激动剂特性。

Role of prostaglandins and specific place in therapy of bimatoprost in the treatment of elevated intraocular pressure and ocular hypertension: A closer look at the agonist properties of bimatoprost and the prostamides.

作者信息

Smid Scott D

机构信息

Discipline of Pharmacology, School of Medical Sciences, Faculty of Health Sciences, University of Adelaide, Adelaide, SA, Australia.

出版信息

Clin Ophthalmol. 2009;3:663-70. doi: 10.2147/opth.s6337. Epub 2009 Dec 29.

DOI:10.2147/opth.s6337
PMID:20054414
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2801635/
Abstract

Bimatoprost is the only representative of a novel class of prostaglandin ethanolamide (prostamide) compounds used therapeutically as an efficacious treatment for glaucoma. The pathways through which bimatoprost works to improve uveoscleral outflow to relieve elevated intraocular pressure are similar to those of the conventional prostaglandins used in glaucoma therapy, with some evidence of a preferential action at the trabecular meshwork. The pharmacology of bimatoprost is however, unclear. Pharmacological evidence supports a specific and distinct receptor-mediated agonist activity of bimatoprost at 'prostamide' receptors, which is selective to the prostamides as a class. However, other studies have reported either activity of bimatoprost at additional prostanoid and nonprostanoid receptors, or a conversion of bimatoprost to metabolites with agonist activity at prostaglandin FP receptors in the human eye. The formation of endogenous prostamides has been demonstrated in vivo, by a novel pathway involving the cyclooxygenase-2-mediated conversion of endogenous cannabinoid (endocannabinoid) substrates. Irrespective of the pharmacology of bimatoprost and the prostamides in general, further studies are needed to determine the biological role and biochemical pathology of prostamides in the human eye, particularly in glaucoma. Such studies may improve our understanding of uveoscleral flow and may offer new treatments for controlling intraocular pressure.

摘要

比马前列素是一类新型前列腺素乙醇酰胺(前列腺酰胺)化合物中唯一用于治疗青光眼的有效代表药物。比马前列素通过改善葡萄膜巩膜外流以缓解眼压升高的作用途径与青光眼治疗中使用的传统前列腺素相似,有证据表明其在小梁网有优先作用。然而,比马前列素的药理学尚不清楚。药理学证据支持比马前列素在“前列腺酰胺”受体上具有特异性且独特的受体介导激动剂活性,这种活性对前列腺酰胺类具有选择性。然而,其他研究报告了比马前列素在其他前列腺素和非前列腺素受体上的活性,或者比马前列素在人眼中转化为在前列腺素FP受体上具有激动剂活性的代谢产物。体内已通过一种涉及环氧化酶-2介导的内源性大麻素底物转化的新途径证明了内源性前列腺酰胺的形成。无论比马前列素和一般前列腺酰胺的药理学如何,都需要进一步研究以确定前列腺酰胺在人眼中,特别是在青光眼中的生物学作用和生化病理学。此类研究可能会增进我们对葡萄膜巩膜外流的理解,并可能为控制眼压提供新的治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826d/2801635/a1a5dd013334/opth-3-663f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826d/2801635/a1a5dd013334/opth-3-663f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826d/2801635/a1a5dd013334/opth-3-663f1.jpg

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