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

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
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; Fruttero, Roberta
File in questo prodotto:
File Dimensione Formato  
2017_dinitroocchio_ACSMCL.pdf

Accesso riservato

Tipo di file: PDF EDITORIALE
Dimensione 749.44 kB
Formato Adobe PDF
749.44 kB Adobe PDF   Visualizza/Apri   Richiedi una copia
ACSMCL_2017_aperto.pdf

Accesso aperto con embargo fino al 30/09/2018

Descrizione: Articolo openaccess
Tipo di file: POSTPRINT (VERSIONE FINALE DELL’AUTORE)
Dimensione 438.67 kB
Formato Adobe PDF
438.67 kB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1650704
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 3
  • ???jsp.display-item.citation.isi??? 3
social impact