Wang R F, Serle J B, Podos S M, Sugrue M F
Department of Ophthalmology, Mount Sinai School of Medicine, New York, NY 10029.
Arch Ophthalmol. 1990 Apr;108(4):511-3. doi: 10.1001/archopht.1990.01070060059049.
L-671,152, a new potent water-soluble inhibitor of human carbonic anhydrase II in vitro, was applied topically to cynomolgus monkey eyes in which glaucoma had been produced by argon laser photocoagulation of the trabecular mesh-work. Intraocular pressure was measured at 0 hours, 0.5 hours, and hourly for 8 hours in eight eyes for 2 baseline days, 1 day receiving the vehicle and 5 days receiving therapy with 2% L-671,152 twice a day, after initial single-dose trials of various concentrations. Intraocular pressure was not significantly different comparing baseline and vehicle-treated days. Significant intraocular pressure reductions occurred from 1 to 8 hours after the first dose, and lasted for at least 16 hours after the second dose. The reduction in intraocular pressure became more pronounced from day 1 to day 5 at each time interval. The mean (+/- SEM) maximum reduction in intraocular pressure was 7.8 +/- 2.1 mm Hg on day 1 and 10.1 +/- 2.4 mm Hg on day 5 at 3 hours after administration, comparing the intraocular pressure in drug-treated and vehicle-treated eyes. L-671,152 has a longer duration of action than does previously studied MK-927 in glaucomatous monkeys. It appears to have great clinical potential.
L-671,152是一种新型强效的人碳酸酐酶II体外水溶性抑制剂，将其局部应用于经氩激光光凝小梁网诱导青光眼的食蟹猴眼中。在进行了各种浓度的初始单剂量试验后，对8只眼睛在2个基线日、1个接受赋形剂的日子以及5个接受2% L-671,152每日两次治疗的日子里，分别在0小时、0.5小时以及之后每小时测量眼压，持续8小时。比较基线日和接受赋形剂治疗日的眼压，差异无统计学意义。首次给药后1至8小时眼压显著降低，第二次给药后至少持续16小时。在每个时间间隔，从第1天到第5天眼压降低更为明显。比较药物治疗组和赋形剂治疗组眼睛的眼压，给药后3小时，第1天眼压平均（±标准误）最大降低7.8±2.1 mmHg，第5天为10.1±2.4 mmHg。在青光眼猴中，L-671,152的作用持续时间比先前研究的MK-927更长。它似乎具有巨大的临床潜力。
