Wang R F, Serle J B, Podos S M, Sugrue M F
Department of Ophthalmology, Mount Sinai School of Medicine, New York, NY.
Arch Ophthalmol. 1991 Sep;109(9):1297-9. doi: 10.1001/archopht.1991.01080090123036.
An investigation was carried out to determine the mechanism by which MK-507 (L-671,152), a water-soluble inhibitor of human carbonic anhydrase II in vitro, reduces intraocular pressure when applied topically to monkey eyes. Intraocular pressure, tonographically measured outflow facility, and fluorophotometrically determined aqueous humor flow were measured before and after therapy in eight normal cynomolgus monkeys. Fifty microliters of 2% MK-507 was instilled in one eye and diluent in the contralateral eye. Baseline values for intraocular pressure, outflow facility, and aqueous humor flow were similar in the drug-treated and diluent-treated control eyes. After therapy, intraocular pressure was significantly (P less than .05) reduced from 1 to 7 hours (eg, 14.0 +/- 1.0 and 15.9 +/- 0.9 mm Hg [mean +/- SEM], treated and control eyes, respectively, at 3 hours). Outflow facility was not significantly (P greater than .40) changed at 3 hours, and aqueous humor flow measured over 5 hours was significantly (P less than .05) reduced (38%) in treated (0.9 +/- 0.1 microL/min) as compared with control eyes (1.5 +/- 0.1 microL/min). The results suggest that MK-507 reduces intraocular pressure by decreasing aqueous humor production.
进行了一项研究，以确定体外人碳酸酐酶II的水溶性抑制剂MK-507（L-671,152）局部应用于猴眼时降低眼压的机制。在八只正常食蟹猴中，于治疗前后测量眼压、眼压描记法测定的房水流畅度以及荧光光度法测定的房水流量。将50微升2%的MK-507滴入一只眼，对侧眼滴入稀释剂。药物治疗眼和稀释剂治疗对照眼中眼压、房水流畅度和房水流量的基线值相似。治疗后，眼压在1至7小时内显著降低（P<0.05）（例如，治疗眼和对照眼在3小时时分别为14.0±1.0和15.9±0.9毫米汞柱[平均值±标准误]）。3小时时房水流畅度无显著变化（P>0.40），与对照眼（1.5±0.1微升/分钟）相比，治疗眼在5小时内测量的房水流量显著降低（P<0.05）（降低38%）（0.9±0.1微升/分钟）。结果表明，MK-507通过减少房水生成来降低眼压。
