To evaluate effects of the topical administration of non-steroidal antiinflammatory drug on anterior uveitis, suprofen eye drop was instilled into the left eye of 10 pigmented rabbits and then experimental anterior uveitis was induced by injecting 750 mocro gram/kg endotoxin of Shigella flexneri serotype 1A into their peritoneal cavities. The pupillary diameters were measured, and cell and flare gradings were recorded in 20 eyes of 10 rabbits for one week at an interval of 12 hours for the first day and then daily. Differences between the treatment and control groups were investigated. All the above parameters showed greatest changes at 12 or 24 hours after the injection of endotoxin and became normal by one week. The treatment and the control groups demonstrated statistically significant difference at 12 hours, day 1, and day 2 as for pupillary diameter and at day 1 and day 2 as for cell and at 12 hours and day 1 as for flare. Thus, it is concluded that prostaglandin plays a role in miosis and the appearance of inflammatory cells and flare in anterior uveitis and the topical administration of non-steroidal anti-inflammatory drug can alleviate signs of anterior uveitis. The specific relationship between leucotriene B4 and polymorphonuclear leucocytes influx was not demonstrated.
Administration, Topical ; Miosis ; Rabbits ; Shigella flexneri ; Suprofen ; Uveitis, Anterior*

We studied the effect of prostaglandin synthesis inhibitor on the ocular hypotensive action of apraclonidine in a prospective, double-masked study. Twenty normal volunteers were studied. Suprofen, cyclooxygenase;nhibitor and apraclonidine were applied to one eye, and normal saline and apraclonidine to the other eye. Intraocular pressure(IOP) was then measured hourly in both eyes for 7 hours. The results showed significant reduction in mean IOP of both eyes one hour after apraclonidine application. The differences of IOP between the suprofen-treated eyes and control eyes were significant at 2 hours following treatment(p<0.05), reached maximum at 3 to 4 hours(p<0.01) and lasted until 7 hours(p<0.05). In suprofentreated eyes, there was less reduction of mean IOP than in control eyes. These results suggest that this reduction of IOP is at least in part mediated by prostaglandins or other cyclooxygenase products, since suprofen inhibits the ocular hypotensive effect of topically applied apraclonidine.
Double-Blind Method ; Healthy Volunteers ; Humans* ; Intraocular Pressure ; Prospective Studies ; Prostaglandin-Endoperoxide Synthases ; Prostaglandins ; Suprofen*

In cataract surgery, the surgically induced miosis complicate the removal of lens materials and implantation of a posterior chamber intraocular lens, which increase the risk of ocular trauma and its associated complication. The refore maintenance of mydriasis during cataract syrgery makes the operation easier and brings a good results. This study was performed in rabbit and human eyes to assess the role of the prostaglandins in surgically induced miosis by observing the reduction of pupillary constriction and by measuring the amount of prostaglandins in aqueous humor when the 1.0% suprofen, cyclo-oxygenase inhibitor, was used, and to assess the effect of suprofen in intraocular pressure. In the results, suprofen inhibits syrgically induced miosis (p value: <0.01, human <0.01) without intraocular pressure change, and for this miosis, prostaglans and for this miosis, prostaglandins are at least partially responsible.
Aqueous Humor ; Cataract ; Constriction ; Humans ; Intraocular Pressure ; Lenses, Intraocular ; Miosis* ; Mydriasis ; Prostaglandin-Endoperoxide Synthases ; Prostaglandins* ; Suprofen

Suprofen eye drop was instilled into one eye of 10 pigmented rabbits and then anterior uveitis was induced by intraperitoneal injection of endotoxin of Shigella flexneri serotype 1A to evaluate the effects of non-steroidal anti-inflammatory drug on endotoxin induced uveitis. The pupillary diameters were measured, and aqueous cell and flare gradings were recorded in 20 eyes of 10 rabbits for one week at an interval of 12 hours for the first 24 hours and then every 24 hours for a week. A difference between the treated and control groups were investigated. All the above parameters showed greatest changes at 12 or 24 hours after injection and became normal by one week. The two groups demonstrated statistically significant difference at 12 hours, day 1 and day 2 as for pupillary diameter, at day 1 and day 2 as for cell and at 12 hours and day 1 as for flare. Thus, it can be concluded that prostaglandins play a role in miosis, in the appearance of inflammatory cells and flare in endotoxin induced uveitis and the topical administration of non-steroidal anti-inflammatory drug can alleviate signs of anterior uveitis. Specific relationship between leukotriene B4 and aqueous cell was not demonstrated.
Administration, Topical ; Animals ; Cell Count ; Endotoxins ; Rabbits ; Shigella flexneri ; Suprofen/*therapeutic use ; Uveitis, Anterior/*drug therapy/pathology

Highly reactive zinc metal was prepared by electrolysis of a N,N-dimethylformamide (DMF) solution containing naphthalene and a supporting electrolyte in a one-compartment cell fitted with a platinum cathode and a zinc anode. This highly reactive electrogenerated zinc (EGZn/Naph) was used for transformation of ethyl 2-bromoacrylate into the corresponding organozinc compound, which can not be achieved by the use of usual zinc metals. Reaction of the organozinc compounds thus prepared with various aryl halides in the presence of 5 mol% of palladium catalyst gave the corresponding cross-coupling products in high yields. These cross-coupling reactions were successfully applied to a synthesis of the precursor of anti-inflammatory agents such as ibuprofen, naproxen, cicloprofen and suprofen.
Anti-Inflammatory Agents, Non-Steroidal/*chemical synthesis ; Catalysis ; Electrolysis ; Ibuprofen/chemical synthesis ; Naphthalenes ; Naproxen/chemical synthesis ; Prodrugs/*chemical synthesis ; Propionic Acids/chemical synthesis ; Suprofen/chemical synthesis ; Zinc/*pharmacology