Abstract
Ocular Hypotensive Activity of a Non-Peptide Bradykinin B2-Receptor Antagonist (WIN-64338) In Dutch-Belt Rabbits- A Case of Poly-Pharmacology in Action
Highlights
Ocular hypertension is a well-recognized and treatable biomarker that is believed to be involved in the etiology of primary open-angle glaucoma, the second leading cause of blindness in the world [1,2,3,4]
Some medications have to be dosed 2-3 times daily to keep the intraocular pressure (IOP) under control and this is associated with reduced compliance and the drugs lose their effectiveness for glaucoma treatment [13,14,15]
When (S)-or (R)-WIN-64338 (50μg [0.16%]) were delivered ivt in Dutch-belted rabbits, a pronounced IOP reduction and a long duration of action was observed with both compounds (Figure 2, Table 2)
Summary
Ocular hypertension is a well-recognized and treatable biomarker that is believed to be involved in the etiology of primary open-angle glaucoma, the second leading cause of blindness in the world [1,2,3,4]. Muscarinic agonists, beta-blockers, alpha-2 agonists, carbonic anhydrase inhibitors and FP-class prostaglandins, and some combinations thereof, are available for lowering IOP of glaucoma patients [5,6,7,8,9,10] While these drugs have proved effective in the reduction and control of ocular hypertension via a number of mechanisms of action, they still have a variety of deficiencies including causing side-effects such as ocular surface burning, hyperemia, ocular foreign-body sensation, ocular allergy, pulmonary and cardiac insufficiency, browe-ache, and iridial and skin hyper-pigmentation [11,12]. The drugs have a slow onset of action and a relatively short duration of action that limits the overall benefit to the patient Due to the latter, some medications have to be dosed 2-3 times daily to keep the IOP under control and this is associated with reduced compliance and the drugs lose their effectiveness for glaucoma treatment [13,14,15]. We investigated receptors and signaling mechanisms potentially mediating the intraocular pressure (IOP)-lowering due to intravitreal (ivt) injection of (S)-WIN-64338, a well-known bradykinin (BK) B2-receptor antagonist
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