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A novel D2-dopaminergic and alpha2-adrenoceptor receptor agonist induces substantial and prolonged IOP decrease in

Jouko Savolainen1, Jarkko Rautio, Roberta Razzetti

  • 1Department of Pharmaceutical Chemistry, University of Kuopio, P.O. Box 1627, FIN-70211 Kuopio, Finland. jouko.savolainen@uku.fi

The Journal of Pharmacy and Pharmacology
|July 5, 2003
PubMed
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A novel D2-dopaminergic/alpha2-adrenoceptor agonist, CHF1035, and its metabolite CHF1024 effectively lowered intraocular pressure (IOP) in rabbits. CHF1035 demonstrated a prolonged IOP-lowering effect, suggesting potential for glaucoma therapy.

Area of Science:

  • Ophthalmology
  • Pharmacology
  • Neuroscience

Background:

  • Glaucoma is a leading cause of irreversible blindness worldwide, characterized by elevated intraocular pressure (IOP).
  • Current treatments aim to reduce IOP, but novel therapeutic agents with improved efficacy and duration are needed.
  • D2-dopaminergic and alpha2-adrenoceptor agonists have shown promise in lowering IOP.

Purpose of the Study:

  • To evaluate the efficacy of a novel D2-dopaminergic/alpha2-adrenoceptor agonist, CHF1035, and its metabolite CHF1024 in reducing intraocular pressure (IOP) in a rabbit model.
  • To compare the IOP-lowering effects of CHF1035, its enantiomers (CHF1800 and CHF1810), and its metabolite CHF1024.
  • To assess the duration of action and safety profile of CHF1035 and CHF1024.

Main Methods:

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  • Topical administration of CHF1035, CHF1024, CHF1800 (+), CHF1810 (-), brimonidine, and saline to rabbits.
  • Measurement of intraocular pressure (IOP) at fixed time intervals post-dosing.
  • Dose-response assessment for CHF1035 (0.01-1.0% w/v) and evaluation of ocular irritation.

    • Main Results:

    • CHF1035 and CHF1024 significantly reduced IOP in treated rabbit eyes.
    • CHF1035 achieved maximum IOP reduction at 5 hours, while CHF1024 showed maximum effect at 3 hours.
    • CHF1035 demonstrated a comparable maximum IOP decrease to brimonidine but with a significantly longer duration of action and no effect on the untreated eye.

    Conclusions:

    • CHF1035 and its metabolite CHF1024 are effective novel agents for lowering intraocular pressure in rabbits.
    • CHF1035 exhibits a sustained IOP-lowering effect, indicating its potential utility in managing glaucoma.
    • The enantiomer CHF1810 (-) showed greater IOP reduction than CHF1800 (+), suggesting stereochemistry influences efficacy.