Novel agonists of melatonin receptors as promising hypotensive and neuroprotective agents for therapy of glaucoma


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Melatonin is a pineal hormone that has a capacity to lower intraocular pressure; it exhibits neuroprotective and antioxidant properties that make it possible to use melatonin in the therapy of glaucoma. Melatonin analogs demonstrating affinity to melatonin receptors are promising candidates for application as antiglaucomatous agents. Chemical modification of the melatonin structure can increase efficiency, bioavailability, and selectivity of melatonin analogs. We have designed and synthesized a number of new 2-oxindole derivatives, the ligands of melatonin MT3 receptors; these analogs are characterized by the ability to lower intraocular pressure in normotensive rabbits and high antioxidant activity against hydroxyl radical and superoxide anion-radical. New ligands significantly exceeding melatonin in antioxidant activity can be also applicable for the development of therapeutic agents for treatment of oxidative stress. The maximal hypotensive effect of the analogs was comparable to and lasted longer than that of melatonin. Combination of these properties suggests potential used of the analyzed melatonin analogs in complex therapy of glaucoma.

作者简介

N. Chesnokova

Moscow Helmholtz Research Institute of Eye Diseases

Email: olval2011@mail.ru
俄罗斯联邦, ul. Sadovaya-Chernogryazskaya, 14/19, Moscow, 105062

O. Beznos

Moscow Helmholtz Research Institute of Eye Diseases

编辑信件的主要联系方式.
Email: olval2011@mail.ru
俄罗斯联邦, ul. Sadovaya-Chernogryazskaya, 14/19, Moscow, 105062

N. Lozinskaya

Chemical Faculty

Email: olval2011@mail.ru
俄罗斯联邦, Moscow, 119991

M. Volkova

Chemical Faculty

Email: olval2011@mail.ru
俄罗斯联邦, Moscow, 119991

E. Zaryanova

Chemical Faculty

Email: olval2011@mail.ru
俄罗斯联邦, Moscow, 119991

N. Zefirov

Chemical Faculty

Email: olval2011@mail.ru
俄罗斯联邦, Moscow, 119991

A. Grigoryev

Moscow Helmholtz Research Institute of Eye Diseases

Email: olval2011@mail.ru
俄罗斯联邦, ul. Sadovaya-Chernogryazskaya, 14/19, Moscow, 105062

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