title: Selective beta 2-adrenoceptor antagonists: derivatives of ICI 118,551 and a binary aryloxypropanolamine.
abstract: Recent studies indicate that selective beta 2-adrenoceptor antagonists may be of use in the treatment of glaucoma. ICI 118,551, its desmethyl-, didesmethyl-, and ethyl- analogues, and a putative highly beta 2-selective binary aryloxypropanolamine (4d) have been evaluated for their ability to inhibit beta-adrenergic-stimulated adenylate cyclase activity in rabbit ciliary process and heart. Potency ratios (Ki heart/Ki ciliary process) were 440 for ICI 118,551; 9.3 for the desmethyl analogue; 8.2 for the didesmethyl analogue; 720 for the ethyl analogue; and 11 for the binary aryloxypropanolamine. The values for the ethyl derivative of ICI 118,551 indicate that it is the most oculoselective beta-adrenoceptor antagonist yet reported.
authors.affiliation: Department of Neurology, Harvard Medical School, Boston, Massachusetts 02114.
authors.forename: J A
authors.initials: JA
authors.lastname: Nathanson
authors.forename: E J
authors.initials: EJ
authors.lastname: Hunnicutt
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D005123:Eye / Q000187:drug effects; D006321:Heart / Q000187:drug effects; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000037:antagonists & inhibitors; D008297:Male; D011412:Propanolamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011817:Rabbits
chemical_list: D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; C026777:ICI 118551; D007545:Isoproterenol