Dihydrolevobunolol is a potent ocular beta-adrenoceptor antagonist.
The ocular beta-adrenoceptor antagonist activity of dihydrolevobunolol (DHLB), the major ocular and systemic metabolite of levobunolol was investigated by determining its ability to block isoproterenol-induced ocular hypotension in normotensive rabbits. Topically-applied 0.001% and 0.01% DHLB virtually abolished the response to isoproterenol, indicating a beta-blocking potency similar to that of timolol. Thus, the ocular metabolism of levobunolol leads to the formation of a highly potent beta-adrenoceptor antagonist that may contribute to its clinical efficacy.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D005123:Eye / Q000187:drug effects*; D005260:Female; D007429:Intraocular Pressure / Q000187:drug effects; D007545:Isoproterenol / Q000037:antagonists & inhibitors / Q000494:pharmacology; D002040:Levobunolol / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D011817:Rabbits
D000319:Adrenergic beta-Antagonists; C015810:dihydrobunolol; D002040:Levobunolol; D007545:Isoproterenol