Binding potencies of 3 new beta 2 specific blockers to beta receptors in the ciliary processes and the possible relevance of these drugs to intraocular pressure control.
The binding potencies of 3 new beta 2 blocking drugs to beta receptors in the ciliary processes were studied by means of radioligand techniques. The drugs studied were IPS339, ICI118,551, and Sandoz L1 32-468. The order of potency of these drugs was IPS339 greater than Sandoz L1 32-468 greater than ICI118,551. The beta 2 dissociation constants (KDs) for these drugs were 0.90 nM, 6.60 nM, and 55 nM respectively. These results are compared with those for other adrenergic agents, including timolol. The potential role of topical beta 2 blockers in glaucoma is discussed.
D000319:Adrenergic beta-Antagonists / Q000378:metabolism* / Q000627:therapeutic use; D000818:Animals; D002924:Ciliary Body / Q000378:metabolism*; D005902:Glaucoma, Open-Angle / Q000188:drug therapy; D011412:Propanolamines / Q000378:metabolism; D011869:Radioligand Assay; D011943:Receptors, Adrenergic, beta / Q000378:metabolism*; D012756:Sheep
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; C026777:ICI 118551; C014898:IPS 339; C042822:LI 32-468