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- W2091581017 abstract "Abstract S-Timolol is an effective anti-glaucoma drug, but has potentially hazardous side effects. Recently, R-timolol, also, has been reported to be effective in lowering elevated intraocular pressure. In the present study, the β-adrenoceptor antagonist activities and binding of RK- and S-enantiomers of timolol have been examined on rat atrial preparations. The β-antagonistic activities were investigated using spontaneously beating rat heart atria. Both timolol enantiomers inhibited (-)-isoprenaline-induced chronotropic action competitively. S-Timolol was about 54 times more potent than R-timolol. The apparent binding affinities of timolol enantiomers to β1 and β2-adrenoceptors were determined by a radioligand binding assay using (-)-[125I]iodocyanopindolol (ICYP) as a marker and CGP 20712 A as a β1- and ICI 118,551 as a β2-adrenoceptor antagonist. Both enantiomers of timolol inhibited ICYP binding in nanomolar concentrations with Hill coefficients near unity. Neither enantiomer showed selectivity between β1- and β2-adrenoceptors, but R-timolol was approximately 30 times less active than S-timolol. It is concluded that R-timolol is a relatively potent non-selective β-adrenoceptor blocking agent, but may possibly exert a more localized β-adrenoceptor action in the eye than S-timolol, thus improving the safety of ocular timolol therapy." @default.
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- W2091581017 date "1989-09-01" @default.
- W2091581017 modified "2023-09-26" @default.
- W2091581017 title "β-Adrenoceptor antagonist activities and binding affinities of timolol enantiomers in rat atria" @default.
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- W2091581017 doi "https://doi.org/10.1111/j.2042-7158.1989.tb06551.x" @default.
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