title: Phenyl-substituted prostaglandins: potent and selective antiglaucoma agents.
abstract: A series of phenyl-substituted analogues of prostaglandin F2 alpha (PGF2 alpha) were prepared and evaluated for ocular hypotensive effect and side effects in different animal models. In addition, the activity of the analogues on FP receptors was studied in vitro. The results were compared with those of PGF2 alpha and its isopropyl ester. The phenyl-substituted PGF2 alpha analogues exhibited good intraocular pressure reducing effect, were more selective, and exhibited a much higher therapeutic index in the eye than PGF2 alpha or its isopropyl ester. The analogues exhibited high activity on FP receptors in a stereoselective manner for the 15 alpha-hydroxyl group.
authors.affiliation: Kabi Pharmacia AB Ophthalmics, Uppsala, Sweden.
authors.forename: B
authors.initials: B
authors.lastname: Resul
authors.forename: J
authors.initials: J
authors.lastname: Stjernschantz
authors.forename: K
authors.initials: K
authors.lastname: No
authors.forename: C
authors.initials: C
authors.lastname: Liljebris
authors.forename: G
authors.initials: G
authors.lastname: Selén
authors.forename: M
authors.initials: M
authors.lastname: Astin
authors.forename: M
authors.initials: M
authors.lastname: Karlsson
authors.forename: L Z
authors.initials: LZ
authors.lastname: Bito
mesh_terms: D000818:Animals; D002415:Cats; D015237:Dinoprost / Q000031:analogs & derivatives* / Q000627:therapeutic use; D005260:Female; D005901:Glaucoma / Q000517:prevention & control*; D007429:Intraocular Pressure / Q000187:drug effects; D008252:Macaca fascicularis; D009119:Muscle Contraction / Q000187:drug effects; D009883:Ophthalmic Solutions / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D011817:Rabbits; D013045:Species Specificity; D013329:Structure-Activity Relationship
chemical_list: D009883:Ophthalmic Solutions; D015237:Dinoprost