| Literature DB >> 21815773 |
Francesca Fabrizi1, Francesco Mincione, Teresa Somma, Gabriele Scozzafava, Fernando Galassi, Emanuela Masini, Francesco Impagnatiello, Claudiu T Supuran.
Abstract
The clinically used sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitor dorzolamide (DRZ), a new sulfonamide CA inhibitor also incorporating NO-donating moieties, NCX250, and isosorbide mononitrate (ISMN) (an NO-donating compound with no CA inhibitory properties) were investigated for their intraocular pressure (IOP) lowering effects in rabbits with carbomer-induced glaucoma. NCX250 was more effective than DRZ or ISMN on lowering IOP, increasing ocular hemodynamics, decreasing the inflammatory processes and ocular apoptosis in this animal model of glaucoma. NO participate to the regulation of IOP in glaucoma, having also antiapoptotic and anti-inflammatory effects. The ophthalmic artery, both systolic and diastolic velocities, were significantly reduced in NCX250-treated eyes in comparison to DRZ treated ones, suggesting thus a beneficial effect of NCX250 on the blood supply to the optic nerve. Combining CA inhibition with NO-donating moieties in the same compound offers an excellent approach for the management of glaucoma.Entities:
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Year: 2011 PMID： 21815773 DOI： 10.3109/14756366.2011.597749
Source DB: PubMed Journal: J Enzyme Inhib Med Chem ISSN： 1475-6366 Impact factor: 5.051