Biochemical and physiological effects of S-32-468, a beta-adrenoceptor antagonist with possible oculoselectivity.
S-32-468, a recently synthesized aryloxymethyl beta-adrenoceptor antagonist, was tested for its ability to inhibit activation of isoproterenol-stimulated adenylate cyclase activity in rabbit and human ciliary process, heart and lung. In both species, S-32-468 was a potent inhibitor of ocular beta-adrenoceptors, with a 9-12 fold selectivity over inhibition of beta-adrenoceptors in cardiac tissue. When applied topically, S-32-468 was more effective than timolol in decreasing intraocular pressure in normal albino rabbits.
Nathanson
J A
JA
D000262:Adenylyl Cyclases / Q000378:metabolism; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D002924:Ciliary Body / Q000201:enzymology; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D007429:Intraocular Pressure / Q000187:drug effects; D007545:Isoproterenol / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008168:Lung / Q000201:enzymology; D008297:Male; D009206:Myocardium / Q000201:enzymology; D011412:Propanolamines / Q000494:pharmacology*; D011817:Rabbits; D013999:Timolol / Q000494:pharmacology
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D013999:Timolol; C042822:LI 32-468; D000262:Adenylyl Cyclases; D007545:Isoproterenol