Wang R F, Serle J B, Podos S M, Surgrue M F
Department of Ophthalmology, Mount Sinai School of Medicine, New York, NY 10029.
Curr Eye Res. 1990 Feb;9(2):163-8. doi: 10.3109/02713689008995202.
MK-927 is a water soluble, potent inhibitor of human carbonic anhydrase (CA) II in vitro. Topical administration of MK-927 reduces intraocular pressure (IOP) in rabbits. Elevated IOP was produced in cynomolgus monkey eyes by argon laser photocoagulation of the trabecular meshwork. IOP was measured at 0 hr, 0.5 hr and hourly for 8 hrs in 8 eyes for two baseline days, one day on vehicle and five days of therapy with 2% MK-927 b.i.d., after initial single-dose trials of various concentrations. IOP was not significantly different comparing baseline and vehicle treated days. Significant (p less than 0.05) reductions of IOP occurred for five days lasting at least 8 hrs after each dosing. At 3 hrs after treatment with vehicle the IOP was 31.6 +/- 3.4 (SE) mm Hg. Maximum reduction of IOP occurred at 3 hrs after application of MK-927, the IOP decreasing from day 1 (19.9 +/- 1.0 mm Hg) to day 5 (16.5 +/- 1.6 mm Hg). MK-927 appears to have great clinical potential.
MK - 927是一种水溶性的、在体外对人碳酸酐酶(CA)II有强效抑制作用的物质。对兔子进行MK - 927局部给药可降低眼内压(IOP)。通过氩激光光凝小梁网在食蟹猴眼中诱导产生高眼压。在进行各种浓度的初始单剂量试验后,对8只眼睛在两个基线日、一天给予赋形剂以及五天每天两次使用2% MK - 927治疗期间,分别在0小时、0.5小时以及之后每小时测量IOP,持续8小时。比较基线日和给予赋形剂治疗日,IOP无显著差异。每次给药后,IOP显著降低(p小于0.05),且持续五天至少8小时。给予赋形剂治疗3小时后,IOP为31.6±3.4(标准误)毫米汞柱。应用MK - 927后3小时IOP降低幅度最大,IOP从第1天(19.9±1.0毫米汞柱)降至第5天(16.5±1.6毫米汞柱)。MK - 927似乎具有巨大的临床潜力。