Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-α-D- glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 1, 2004, Pages 225-229

  Winum, Jean Yves ^a   Casini, Angela ^b   Mincione, Francesco ^c   Starnotti, Michele ^d   Montero, Jean Louis ^a   Scozzafava, Andrea ^b   Supuran, Claudiu T ^b  

^a UNIV MONTPELLIER   (France)

^b UNIVERSITY OF FLORENCE   (Italy)

^c Ospedale di Pescia   (Italy)

^d Clinica Oculistica   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ACETAZOLAMIDE; AMMONIUM CHLORIDE; ANTIGLAUCOMA AGENT; BRINZOLAMIDE; CARBONATE DEHYDRATASE I; CARBONATE DEHYDRATASE II; CARBONATE DEHYDRATASE INHIBITOR; DICLOFENAMIDE; DORZOLAMIDE; METHAZOLAMIDE; MONOSACCHARIDE; N (4 SULFAMOYLPHENYL) ALPHA 5 DEXTRO XYLOPYRANOSYLAMINE; N (4 SULFAMOYLPHENYL) ALPHA DEXTRO ARABINOPYRANOSYLAMINE; N (4 SULFAMOYLPHENYL) ALPHA DEXTRO FUCOSYLAMINE; N (4 SULFAMOYLPHENYL) ALPHA DEXTRO GALACTOPYRANOSYLAMINE; N (4 SULFAMOYLPHENYL) ALPHA DEXTRO GLUCOPYRANOSYLAMINE; N (4 SULFAMOYLPHENYL) ALPHA DEXTRO MANNOPYRANOSYLAMINE; N (4 SULFAMOYLPHENYL) ALPHA DEXTRO RIBOPYRANOSYLAMINE; N (4 SULFAMOYLPHENYL) ALPHA LEVO RHAMNOSYLAMINE; SULFANILAMIDE; SULFONAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AQUEOUS HUMOR; ARTICLE; CHEMICAL REACTION; CONTROLLED STUDY; DRUG EFFECT; DRUG SOLUBILITY; DRUG SYNTHESIS; ENZYME INHIBITION; GLAUCOMA; HYPERTENSION; IC 50; INTRAOCULAR PRESSURE; MAMMAL; NONHUMAN; RABBIT; REACTION ANALYSIS;

ANIMALIA; MAMMALIA; ORYCTOLAGUS CUNICULUS;

EID: 0347517808     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.09.063     Document Type: Article

References (22)

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21. Adult male New Zealand albino rabbits weighing 3-3.5 kg were used in the experiments (three animals were used for each inhibitor studied). The experimental procedures conform to the Association for Research in Vision and Ophthalmology Resolution on the use of animals. The rabbits were kept in individual cages with food and water provided ad libitum. The animals were maintained on a 12 h/12 h light/dark cycle in a temperature controlled room, at 20-24°C.
22. IOP was measured using a Tono-Pen XL digital instrument (Medtronic Solan, USA). The pressure readings were matched with two-point standard pressure measurements at least twice each day using a Digilab Calibration verifier. All IOP measurements were done by the same investigator with the same tonometer. One drop of 0.2% oxybuprocaine hydrochloride (novesine, Sandoz) diluted 1:1 with saline was instilled in each eye immediately before each set of pressure measurements. IOP was measured three times at each time interval, and the means reported. IOP was measured first immediately before drug administration, then at 30 min after the instillation of the pharmacological agent, and then each 30 min for a period of 4-6 h. For all IOP experiments drug was administered to only one eye, leaving the contralateral eye as an untreated control. The ocular hypotensive activity is expressed as the average difference in IOP between the treated and control eye, in this way minimizing the diurnal, seasonal and interindividual variations commonly observed in the rabbit.