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A cyclic AMP phosphodiesterase inhibitor, 8'-pivaloyloxymethyl ester (POM-ester) of griseolic acid, lowers rabbit intraocular pressure.

Abstract
The effects of griseolic acid (GA), a cyclic-AMP phosphodiesterase (PDE) inhibitor, and its 8'-pivaloyloxymethyl (POM) ester on intraocular pressure (IOP) in rabbits were investigated. When 50 microliters of 1 and 2% GA POM ester solutions were topically applied to one eye in normal rabbits, significant IOP decreases were detected at 2 hrs and at 1 to 5 hrs, respectively. Other than ocular hypotension, no other ocular effects were detected locally even after administration of 2% GA POM ester. A more marked reduction in IOP occurred after the intravitreal injection of the GA POM ester. IOP was also reduced when GA was used in an intravitreal injection but not when it was topically applied. The difference in permeability between GA and GA POM ester across the corneal epithelium may explain why GA failed to reduced IOP following topical administration. GA and the GA POM ester inhibited cAMP PDE in rabbit ciliary body at low concentrations, the I50 being 0.075 microM and 2.4 microM, respectively, with 0.25 microM cAMP as substrate. GA and the GA POM ester markedly increased cAMP levels in vitro in iris-ciliary body specimens. Possibly, GA POM ester or its analogues may represent a new mechanistic class of ocular hypotensive agents.
AuthorsH K Mishima, Y Kiuchi, T Yokoyama, T Yasumoto, M Yamazaki
JournalCurrent eye research (Curr Eye Res) Vol. 10 Issue 9 Pg. 817-22 (Sep 1991) ISSN: 0271-3683 [Print] England
PMID1665121 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • griseolic acid 8'-pivaloyloxymethyl ester
  • griseolic acid
  • 3',5'-Cyclic-AMP Phosphodiesterases
  • Cyclic GMP
  • Adenosine
Topics
  • 3',5'-Cyclic-AMP Phosphodiesterases (antagonists & inhibitors)
  • Adenosine (analogs & derivatives, pharmacokinetics, pharmacology)
  • Animals
  • Ciliary Body (drug effects, enzymology)
  • Cornea (metabolism)
  • Cyclic GMP (metabolism)
  • Intraocular Pressure (drug effects)
  • Iris (metabolism)
  • Male
  • Permeability
  • Rabbits
  • Vitreous Body (drug effects)

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