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2000

Protocols for Access to and Dose Selection of Selected IOP-Lowering Drugs

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Described herein are high-level protocols to access selected small molecules with IOP-lowering properties when topically dosed as ophthalmic formulations, as well as dose selection for evaluation in appropriate animal models. Sources are provided for commercially available drugs, and high-level synthetic protocols are described for agents that are not commercially available. The agents described are approved for use in humans or have demonstrated robust pre-clinical activity. These are drawn from a diverse range of pharmacological classes, such as prostaglandin analogs, betaadrenergic antagonists, carbonic anhydrase inhibitors, alpha-adrenergic agonists, and dual-activity prostaglandin-NO donors. Their physiological mechanisms of action have been characterized by the suppression of aqueous humor (AH) inflow, enhancement of AH conventional or uveoscleral outflow, and reduction of episcleral venous pressure.

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