May 2007
Volume 48, Issue 13
ARVO Annual Meeting Abstract  |   May 2007
A Comparison of in vitro Receptor Binding of Glucocorticoids
Author Affiliations & Notes
  • F. E. Kane
    Scientific Affairs, Alimera Sciences Inc, Alpharetta, Georgia
  • K. E. Green
    Scientific Affairs, Alimera Sciences Inc, Alpharetta, Georgia
  • A. Weissman
    Chief Technical Officer, Novascreen Biosciences, a Caliper Life Science Co., Hanover, Maryland
  • Footnotes
    Commercial Relationships F.E. Kane, Alimera Sciences Inc., E; K.E. Green, Alimera Sciences Inc., E; A. Weissman, Novascreen Biosciences, E.
  • Footnotes
    Support None.
Investigative Ophthalmology & Visual Science May 2007, Vol.48, 106. doi:
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      F. E. Kane, K. E. Green, A. Weissman; A Comparison of in vitro Receptor Binding of Glucocorticoids. Invest. Ophthalmol. Vis. Sci. 2007;48(13):106.

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      © ARVO (1962-2015); The Authors (2016-present)

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There is increasing interest in the use of glucocorticoids for the treatment of exudative and neovascular eye diseases. Data from clinical studies of sustained release dexamethasone (DEX, Posurdex®), immediate release triamcinolone acetonide (TA) and sustained release fluocinolone acetonide (FA, Retisert®) suggest that glucocorticoids may differ in their efficacy and safety which could be the result of differences in potency. The purpose of this study was to compare the in vitro receptor binding of FA to DEX and TA.


A human recombinant glucocorticoid cell membrane preparation was used for comparative binding assays after the method of DaHan, 1994. 3H-Dexamethasone (1 nM) was allowed to competitively bind to the receptors at 0° C. for 16 hours in the presence and absence of varying concentrations of FA, DEX or TA (n= 2 at each concentration). The reaction was terminated by rapid filtration through glass fiber filters. Specific radioactivity trapped on the filters was determined by liquid scintillation photometry.


The Ki values for all three glucocorticoids demonstrated they had approximately similar potencies at the human glucocorticoid receptor  


In view of the very similar affinities of FA and TA for the human glucocorticoid receptor, differences in efficacy are likely to be due more to pharmacokinetic rather than pharmacodynamics differences. DEX appears to be slightly less potent based on receptor binding. The relevance of these findings will be discussed.

Keywords: corticosteroids • drug toxicity/drug effects • retina 

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