Primary open angle glaucoma is the second most common cause of blindness worldwide. Nitric oxide has recently received particular attention as a potential antiglaucoma agent. In this work, gem-dinitroalkyl benzenes are evaluated for their capability to act as a new class of IOP lowering agents. These derivatives have been endowed with a variety of NO-release capacities and found to relax contracted rat aorta strips in a concentration-dependent manner. They have been studied for their IOP-lowering activity in a transient ocular hypertensive rabbit model at 1% dose. The most effective IOP-lowering products were compounds 9−11 and 13, whose activity was similar to that of Molsidomine 120 min after administration. Compounds 9 and 13 were selected for evaluation using carbomer-induced glaucoma as the chronic model of IOP. They cause a significant reduction in IOP in the first 24 h, and their activity is maintained over 5 days, displaying a Molsidomine-like profile

gem-Dinitroalkyl Benzenes: A Novel Class of IOP-Lowering Agents for the Treatment of Ocular Hypertension

BLANGETTI, Marco;ROLANDO, Barbara;MARINI, Elisabetta;CHEGAEV, Konstantin;GUGLIELMO, Stefano;LAZZARATO, Loretta
;
FRUTTERO, Roberta
2017-01-01

Abstract

Primary open angle glaucoma is the second most common cause of blindness worldwide. Nitric oxide has recently received particular attention as a potential antiglaucoma agent. In this work, gem-dinitroalkyl benzenes are evaluated for their capability to act as a new class of IOP lowering agents. These derivatives have been endowed with a variety of NO-release capacities and found to relax contracted rat aorta strips in a concentration-dependent manner. They have been studied for their IOP-lowering activity in a transient ocular hypertensive rabbit model at 1% dose. The most effective IOP-lowering products were compounds 9−11 and 13, whose activity was similar to that of Molsidomine 120 min after administration. Compounds 9 and 13 were selected for evaluation using carbomer-induced glaucoma as the chronic model of IOP. They cause a significant reduction in IOP in the first 24 h, and their activity is maintained over 5 days, displaying a Molsidomine-like profile
2017
8
1054
1059
gem-Dinitroalkyl benzenes, nitric oxide, glaucoma, ocular hypertension
Blangetti, Marco; Rolando, Barbara; Marini, Elisabetta; Chegaev, Konstantin; Guglielmo, Stefano; Lazzarato, Loretta; Laura, Lucarini; Emanuela, Masini...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1650704
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