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Preclinical efficacy of travoprost, a potent and selective FP prostaglandin receptor agonist.
TLDR
Topical application of travoprost was well tolerated in rabbits, cats and monkeys, causing no ocular irritation or discomfort at doses up to 1 microg, and has the ocular hypotensive efficacy of PGF2alpha isopropyl ester but with less severe ocular side effects. Expand
Evaluation of inducible nitric oxide synthase in glaucomatous optic neuropathy and pressure-induced optic nerve damage.
PURPOSE To determine whether inducible nitric oxide synthase (NOS-2) is involved in glaucomatous optic neuropathy. METHODS Chronic elevation of rat intraocular pressure (IOP) leading to optic nerveExpand
Agonists at the serotonin receptor (5-HT(1A)) protect the retina from severe photo-oxidative stress.
TLDR
5-HT(1A) agonists provided potent and complete functional and structural protection and AL-8309B is under evaluation in the clinic and may be useful in treating age-related macular degeneration. Expand
Identification and characterization of the ocular hypotensive efficacy of travoprost, a potent and selective FP prostaglandin receptor agonist, and AL-6598, a DP prostaglandin receptor agonist.
TLDR
Clinical studies show that travoprost 0.004% (isopropyl ester) provided intraocular pressure control superior to timolol 0.5% when used as monotherapy in patients with open-angle glaucoma or ocular hypertension, and AL-6598 0.01% provided a sustained intraocular Pressure reduction with q.i.d. application. Expand
Evaluation of the Ocular Hypotensive Response of Serotonin 5-HT1A and 5-HT2 Receptor Ligands in Conscious Ocular Hypertensive Cynomolgus Monkeys
TLDR
Compounds that function as efficient agonists at 5-HT2 receptors should be considered as potential agents for the control of intraocular pressure in the treatment of ocular hypertension and glaucoma in humans. Expand
The hydrolysis of the prostaglandin analog prodrug bimatoprost to 17-phenyl-trinor PGF2alpha by human and rabbit ocular tissue.
TLDR
Separate in vitro studies clearly show that both bimatoprost and 17-phenyl-trinor PGF(2alpha) have affinity for and are agonists at the human FP receptor, and strongly suggests that the ocular hypotensive effect of bim atoprost can be attributed to its activity as a prostaglandin receptor agonist either directly or through its role as a prodrug. Expand
Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.
TLDR
Intraocular administration of 300 microg of 6d and 7d to ocular hypertensive monkeys was shown to reduce intraocular pressure, and compounds such as 6d should demonstrate minimal central effects at potentially useful therapeutic doses and offer useful leads for further development. Expand
Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.
A series of 8-substituted benzodifuran analogs was prepared and evaluated for 5-HT(2A) receptor binding and activation. Several compounds containing ether and ester functionality were found to beExpand
Water-soluble PDE4 inhibitors for the treatment of dry eye.
TLDR
The development of a novel series of water-soluble PDE4 inhibitors led to the discovery of coumarin 18, which is effective in a rabbit model of dry eye and a tear secretion test in rats. Expand
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