Preclinical pharmacology, ocular tolerability and ocular hypotensive efficacy of a novel non-peptide bradykinin mimetic small molecule.

We sought to characterize the ocular pharmacology, tolerability and intraocular pressure (IOP)-lowering efficacy of FR-190997, a non-peptidic bradykinin (BK) B2-receptor agonist. FR-190997 possessed a relatively high receptor binding affinity (Ki = 27 nM) and a high in vitro potency (EC50 = 18.3 ± 4.

The disposition and bioavailability of 35S-GSH from 35S-GSSG in BSS PLUS in rabbit ocular tissues.

The purpose of this study was to evaluate the biodistribution and uptake of 35S-GSH into intraocular tissues following the administration of BSS PLUS containing 35S-GSSG by either an anterior chamber or intravitreal injection. This study evaluated the disposition and uptake of the 35S-radiolabel, the intracellular concentrations of 35S-GSH from extracellular 35S-GSSG, and the percentage of 35S-GSH to the total cellular GSH pool. Glutathione was analyzed by high-performance liquid chromatography (HPLC) using fluorescence detection after derivitizing the thiols in situ with monobromobimane.