The effect of the Rho-associated protein kinase inhibitor, HA-1077, in the rabbit ocular hypertension model induced by water loading.
OBJECTIVE
The aim of this study was to investigate the intraocular pressure (IOP)-lowering effect of a new anti-glaucoma drug, the Rho-associated protein kinase (ROCK) inhibitor, HA-1077, in a rabbit ocular hypertension model.


METHODS
Experiments were carried out in 18 male New Zealand white rabbits, with ocular hypertension induced by water loading. Animals were divided into three groups followed by topical administration of 1 mM, 2 mM, and 3 mM HA-1077 in the left eye. As a control, phosphate buffered saline was administered in the opposite eye.


RESULTS
After administration of HA-1077 eye drops, there was a significant time- and dose-dependent decrease of the IOP. While minor conjunctival injection was seen in a few cases, no abnormalities of the anterior chamber or fundus were observed.


CONCLUSIONS
This is the first report of the effect of the ROCK inhibitor, HA-1077, on the IOP in an ocular hypertension model. Study results indicated that HA-1077 has a strong IOP-lowering effect.
Fukunaga
Takaki
T
Department of Ophthalmology, Graduate School of Medicine, Mie University, Tsu, Mie, Japan.
Ikesugi
Kengo
K
Nishio
Masahiro
M
Sugimoto
Masahiko
M
Sasoh
Mikio
M
Hidaka
Hiroyoshi
H
Uji
Yukitaka
Y
D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology; D000287:Administration, Topical; D000818:Animals; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D007429:Intraocular Pressure / Q000187:drug effects*; D008297:Male; D009798:Ocular Hypertension / Q000188:drug therapy*; D009883:Ophthalmic Solutions / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D011817:Rabbits; D013312:Stress, Physiological; D013997:Time Factors; D014867:Water; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
D009883:Ophthalmic Solutions; D047428:Protein Kinase Inhibitors; D014867:Water; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D054460:rho-Associated Kinases; C049347:fasudil