An important task of pharmacology is to find effective agents to improve retinal microcirculation and resistance to ischemia. The purpose of the study is to pharmacologically evaluate the retinoprotective effect of 2-ethyl-3-hydroxy-6-methylpyridine nicotinate in a rat model of retinal ischemia–reperfusion. A retinal ischemia–reperfusion model was used, in which an increase in intraocular pressure (IOP) to 110 mmHg was carried out within 30 min. The retinoprotective effect of 2-ethyl-3-hydroxy-6-methylpyridine nicotinate at a dose of 3.8 mg/kg, in comparison with nicotinic acid at a dose of 2 mg/kg and emoxipine at a dose of 2 mg/kg, was estimated by the changes in the eye fundus during ophthalmoscopy, the retinal microcirculation level with laser Doppler flowmetry (LDF), and electroretinography (ERG) after 72 h of reperfusion. The use of 2-ethyl-3-hydroxy-6-methylpyridine nicotinate prevented the development of ischemic injuries in the fundus and led to an increase in the retinal microcirculation level to 747 (median) (lower and upper quartiles: 693;760) perfusion units (p = 0.0002) in comparison with the group that underwent no treatment. In the group with the studied substance, the b-wave amplitude increased significantly (p = 0.0022), and the b/a coefficient increased reliably (p = 0.0002) in comparison with the group with no treatment. Thus, 2-ethyl-3-hydroxy-6-methylpyridine nicotinate has established itself as a potential retinoprotector.
Исследовано нейропротективное действие агониста имидазолиновых рецепторов типов I и II, 3-(1H-бензимидазол-2-ил)-1,2,2-триметилциклопентанкарбоновой кислоты, в дозе 50 мг/кг в сравнении с пикамилоном в дозе 30 мг/кг на модели ишемической нейропатии зрительного нерва у крыс-самцов линии Wistar. В эксперименте выявлено, что 3-(1H-бензимидазол-2-ил)-1,2,2-триметилциклопентанкарбоновая кислота предотвращает развитие ишемической нейропатии зрительного нерва, вызванной введением неселективного ингибитора NO-синтазы N-нитро-L-аргинин-метилового эфира (L-NAME) в дозе 12,5 мг/кг в течение 28 сут, и однократным повышением внутриглазного давления (ВГД) до 110 мм рт. ст., в большей степени, чем пикамилон. У крыс в группе с коррекцией 3-(1H-бензимидазол-2-ил)-1,2,2-триметилциклопентанкарбоновой кислотой удельное количество ядер нейронов в наружном ядерном слое достоверно выше на 15,0 % (p < 0,05), в сравнении с группой животных с введением пикамилона; на 33,3 % (p < 0,05), в сравнении с группой с моделированием патологии, что свидетельствует о сохранении их жизнеспособности. Обнаруженные протективные эффекты подтверждены результатами офтальмоскопии и гистологических исследований на 29 сут эксперимента.
Introduction:Retinoprotective effects of non-selective imidazoline receptor agonists: potassium salt of С7070; sodium salt of С7070; С7070 processed with CO 2 -were investigated in comparison with C7070 on the retinal ischemia-reperfusion model in rats.
Materials and methods:The protective effects of the substances were evaluated by using ophthalmoscopy, laser Doppler flowmetry, electroretinography, histological and morphometric studies of retinal layers.
Results and discussion:The most pronounced retinoprotective effect was observed in potassium salt of C7070 at a dose of 10 mg/kg, which expresses in approaching the normal eye fundus image, achieving the target values of the retinal blood flow, b/a coefficient, and reaching the norm values of morphometric indicators. A less pronounced protective effect was found in sodium salt of C7070 at a dose of 10 mg/kg, which expresses in a 71% decrease (p < 0.05) in semi-quantitative assessment of the eye fundus changes, an increase in the retinal blood flow level by 70.4% (p < 0.05), in b/a by 94% (p < 0.05) in comparison with the group without correction, and reaching the norm of the morphometric indicators. A retinoprotective effect of the substance C7070 processed with CO 2 at a dose of 10 mg/kg is inferior to that of the sodium salt of C7070.
Conclusion:The retinoprotective activity of the substances is expressed in descending order: potassium salt of С7070 (10 mg/kg) ≈ С7070 (50 mg/kg) > sodium salt of С7070 (10 mg/kg) > С7070 processed with CO 2 (10 mg/kg) ≈ С7070 (10 mg/kg). Injections of glibenclamide leveled the neuroretinoprotective effects of the substances to varying degrees, which confirmed the participation of ATP-dependent potassium channels in the implementation of these effects.
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