Selective β2-adrenoceptor antagonists: derivatives of ICI 118,551 and a binary aryloxypropanolamine
- 1 November 1988
- journal article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 40 (11), 803-805
- https://doi.org/10.1111/j.2042-7158.1988.tb05177.x
Abstract
Recent studies indicate that selective β2-adrenoceptor antagonists may be of use in the treatment of glaucoma. ICI 118,551, its desmethyl-, didesmethyl-, and ethyl- analogues, and a putative highly β2-selective binary aryloxypropanolamine (4d) have been evaluated for their ability to inhibit β-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 β-adrenoceptor antagonist yet reported.Keywords
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