Effect of WIN 55212-2, a cannabinoid receptor agonist, on aqueous humor dynamics in monkeys

Arch Ophthalmol. 2003 Jan;121(1):87-90. doi: 10.1001/archopht.121.1.87.

Abstract

Objective: To evaluate the effects of WIN 55212-2, a cannabinoid receptor agonist, on intraocular pressure and aqueous humor dynamics in normal monkeys and monkeys with glaucoma.

Methods: Intraocular pressure was measured prior to and up to 6 hours after the topical administration of WIN 55212-2 to 1 eye of 5 normal monkeys and to the glaucomatous eye of 8 monkeys with unilateral laser-induced glaucoma. Tonographic outflow facility and fluorophotometric flow rates of aqueous humor were measured in 6 normal monkeys before and after treatment.

Results: In normal monkeys, a single dose of WIN 55212-2 reduced intraocular pressure for 4, 5, or 6 hours, with a maximum reduction of 1.4 +/- 0.4 (mean +/- SEM) mm Hg, 2.9 +/- 0.4 mm Hg, and 3.4 +/- 0.6 mm Hg following the 0.07%, 0.2%, and 0.5% concentrations, respectively (P =.08). In 8 glaucomatous monkey eyes, the ocular hypotensive effect was maintained for 5 days with twice-daily administration of 0.5% WIN 55212-2. Outflow facility was unchanged (P =.34) and aqueous humor flow was decreased by 18% (P =.04) in the treated eyes compared with vehicle-treated contralateral control eyes in normal monkeys.

Conclusions: WIN 55212-2, a cannabinoid agonist at the CB(1) receptor, reduces intraocular pressure in both normal and glaucomatous monkey eyes. A decrease of aqueous flow appears to account for the intraocular pressure reduction in normal monkey eyes.

Clinical relevance: Cannabinoid agonists at the CB(1) receptor, a new class of antiglaucoma agents that is different from currently used clinical drugs, may have clinical potential.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Administration, Topical
  • Animals
  • Aqueous Humor / metabolism*
  • Benzoxazines
  • Calcium Channel Blockers / administration & dosage*
  • Cannabinoids / agonists
  • Disease Models, Animal
  • Female
  • Fluorophotometry
  • Glaucoma / drug therapy*
  • Glaucoma / metabolism
  • Intraocular Pressure / drug effects*
  • Laser Coagulation
  • Macaca fascicularis
  • Morpholines / administration & dosage*
  • Naphthalenes / administration & dosage*
  • Ophthalmic Solutions
  • Receptors, Cannabinoid
  • Receptors, Drug / agonists*
  • Tonometry, Ocular
  • Trabecular Meshwork / surgery

Substances

  • Benzoxazines
  • Calcium Channel Blockers
  • Cannabinoids
  • Morpholines
  • Naphthalenes
  • Ophthalmic Solutions
  • Receptors, Cannabinoid
  • Receptors, Drug
  • (3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone