A comparison of L-671,152 and MK-927, two topically effective ocular hypotensive carbonic anhydrase inhibitors, in experimental animals.
@article{Sugrue1990ACO, title={A comparison of L-671,152 and MK-927, two topically effective ocular hypotensive carbonic anhydrase inhibitors, in experimental animals.}, author={Michael F. Sugrue and Pierre J. Mallorga and Harvey Schwam and John J. Baldwin and Gerald S. Ponticello}, journal={Current eye research}, year={1990}, volume={9 6}, pages={ 607-15 } }
L-671,152 is a water-soluble, carbonic anhydrase inhibitor structurally similar to MK-927, a carbonic anhydrase inhibitor that, on topical administration, lowers the intraocular pressure (IOP) of experimental animals and humans. L-671,152 was more potent than MK-927 at inhibiting purified, human erythrocyte carbonic anhydrase II in vitro, as reflected in their respective IC50 values of 0.16 nM and 1.19 nM. Both compounds were compared for topical, ocular hypotensive activity in pigmented…
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References
SHOWING 1-10 OF 23 REFERENCES
L‐662,583 is a topically effective ocular hypotensive carbonic anhydrase inhibitor in experimental animals
- Medicine, BiologyBritish journal of pharmacology
- 1990
The ocular normotensive, albino rabbit was much less susceptible than the ocular hypertensive rabbit to the intraocular pressure lowering effect of topically applied L‐662,583, with a 2% solution maximally decreasing intraocular Pressure by 2.3 mmHg.
Local tolerance and activity of MK-927, a novel topical carbonic anhydrase inhibitor.
- MedicineArchives of ophthalmology
- 1988
Local tolerance of 2% MK-927 was acceptable and supports further clinical trials in patients and significant intraocular pressure-lowering activity was noted when comparing IOP four hours after first dose with that 20 hours predose in the treated eye of subjects receiving MK- 927.
On the pharmacology of L-645,151: a topically effective ocular hypotensive carbonic anhydrase inhibitor.
- Biology, ChemistryThe Journal of pharmacology and experimental therapeutics
- 1985
Preclinical studies reveal that L-645,151 is the most potent, topically effective ocular hypotensive carbonic anhydrase inhibitor described to date.
The effect of MK-927, a topical carbonic anhydrase inhibitor, on IOP in glaucomatous monkeys.
- Medicine, EngineeringCurrent eye research
- 1990
Topical administration of MK-927 reduces intraocular pressure (IOP) in rabbits and appears to have great clinical potential after initial single-dose trials of various concentrations.
Chemical and pharmacological properties of MK-927, a sulfonamide carbonic anhydrase inhibitor that lowers intraocular pressure by the topical route.
- Chemistry, BiologyExperimental eye research
- 1990
MK-927: a topically effective carbonic anhydrase inhibitor in patients.
- MedicineArchives of ophthalmology
- 1989
The effects on intraocular pressure of the novel topical carbonic anhydrase inhibitor MK-927 were investigated for the first time in patients in a two-center, double-masked, randomized, placebo-controlled, two-period crossover study in patients with bilateral primary open angle glaucoma or ocular hypertension.
MK-927: a topical carbonic anhydrase inhibitor. Dose response and duration of action.
- MedicineArchives of ophthalmology
- 1990
The dose response to a single topical administration of the carbonic anhydrase inhibitor MK-927 was investigated in 24 patients with primary open angle glaucoma or ocular hypertension and appeared to lower intraocular pressure in a dose-dependent fashion.
Ocular distribution studies of the topical carbonic anhydrase inhibitors L-643,799 and L-650,719 and related alkyl prodrugs.
- Chemistry, BiologyJournal of ocular pharmacology
- 1988
The ocular distribution of the carbonic anhydrase inhibitors 6-hydroxybenzothiazide-2-sulphonamide and L-650,719 has been investigated in albino rabbits after conjunctival administration of these compounds or related alkyl prodrugs.
Carbonic anhydrase inhibitor side effects. Serum chemical analysis.
- MedicineArchives of ophthalmology
- 1977
Patients with chronic glaucoma complained of a symptom-complex of malaise, fatigue, weight loss, depression, anorexia, and loss of libido, which has found most commonly to threaten continuation of therapy.
Carbonic anhydrase: General perspective and advances in glaucoma research
- Chemistry
- 1987
The chemistry and physiology of carbonic anhydrase are reviewed in relation to pharmacological progress in the development of sulfonamide inhibitors. The major organ systems are briefly dicussed.…