Selective beta 2-adrenoceptor antagonists: derivatives of ICI 118,551 and a binary aryloxypropanolamine

J Pharm Pharmacol. 1988 Nov;40(11):803-5. doi: 10.1111/j.2042-7158.1988.tb05177.x.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adrenergic beta-Antagonists / chemical synthesis*
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Eye / drug effects
  • Heart / drug effects
  • In Vitro Techniques
  • Isoproterenol / antagonists & inhibitors
  • Male
  • Propanolamines / chemical synthesis*
  • Propanolamines / pharmacology*
  • Rabbits

Substances

  • Adrenergic beta-Antagonists
  • Propanolamines
  • ICI 118551
  • Isoproterenol