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• W2012624430 abstract "Preclinical studies of brimonidine show that it is a potent α2-adrenoceptor agonist that is 1000-fold more selective for the α2- vs. the α1-adrenoceptor, and is 7–12-fold more α2-selective than clonidine and 23- to 32-fold more α2-selective than apraclonidine (p-aminoclonidine). Brimonidine decreased intraocular pressure (IOP) in various animal models but, unlike apraclonidine, brimonidine was not mydriatic. The site and pharmacology of the IOP response depends on the animal species. In rabbits, the IOP response to brimonidine is mediated by an ocular α2-adrenoceptor while in monkeys, a central nervous system (CNS) ‘imidazoline’ receptor appears to be involved. Brimonidine decreased IOP by suppressing the rate of aqueous humor flow and enhancing uveoscleral outflow. Topical brimonidine resulted in posterior segment drug levels adequate to activate α2-adrenoceptors, but was not vasoconstrictive in a model designed to assess the vasoactivity of the human retinal microvasculature. Brimonidine protected the rat optic nerve from secondary damage following mechanical injury to the optic nerve and was nontoxic in an array of experiments designed to evaluate ocular and organ toxicity. Taken together, the high α2-adrenoceptor selectivity, ocular hypotensive efficacy, retinal bioavailability and neuroprotective properties make brimonidine an important addition to the field of antiglaucoma agents." @default.
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• W2012624430 date "1996-11-01" @default.
• W2012624430 modified "2023-10-14" @default.
• W2012624430 title "Preclinical evaluation of brimonidine" @default.
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• W2012624430 doi "https://doi.org/10.1016/s0039-6257(96)82027-3" @default.
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