PMID: 6115904Apr 1, 1981

How beta2-selective is the adrenoceptor antagonist drug, IPS 339?

The Journal of Pharmacy and Pharmacology
S R O'Donnell, K Walduck

Abstract

Schild plots for the compound (t-butylamino-3-ol-2-propyl)oximino-9-fluorene (IPS 399) have been obtained on isolated intrinsic tone trachea and atria (rate) og guinea-pigs. Alpha-Adrenoceptors and uptakes were inhibited. The Schild plots for IPS 339 on trachea (fenoterol as agonist) and on atria (noradrenaline as agonist) were not superimposed suggesting that IPS 339 was beta2-selective. The slopes of the Schild plots obtained on intrinsic tone tracheal preparations (isoprenaline or fenoterol as agonist), although greater than 1.0, were not significantly different from that on atria (noradrenaline as agonist). From the average separation of these Schild plots on trachea and atria IPS 339 was assessed to be only 3.3 times more active on beta2- than on beta1-adrenoceptors. The experiments in the literature which showed a high beta2-selectivity for IPS 339 (155 fold) were carried out on carbachol-contracted tracheal preparations (isoprenaline as agonist) and the Schild plot obtained had a very low slope which was quite different from that on atria. Therefore, the results illustrate how the quantitative estimate of the selectivity of a beta-adrenoceptor antagonist can be misleading when Schild plots with different slopes are compa...Continue Reading

Citations

Jan 1, 1984·Graefe's Archive for Clinical and Experimental Ophthalmology = Albrecht Von Graefes Archiv Für Klinische Und Experimentelle Ophthalmologie·C J SchmittN N Share
Sep 2, 1983·European Journal of Pharmacology·N L Brown, M Worcel
Apr 1, 1984·Acta Pharmacologica Et Toxicologica·R KlysnerK Winther
Sep 1, 1983·The Journal of Pharmacy and Pharmacology·B CostinJ C Wanstall

Related Concepts

IPS 339, monohydrochloride, (+-)-isomer
Adrenergic beta-Antagonists
Cavia porcellus
Right Atrial Structure
Propanolamines
Norepinephrine Receptors
Beta-adrenergic receptor
Trachea

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