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The beta‐adrenoceptor antagonist carteolol and its metabolite 8‐ hydroxycarteolol have different intrinsic sympathomimetic activities.
Author(s) -
Jasper J.R.,
Michel MC,
Insel PA
Publication year - 1990
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1990.tb05477.x
Subject(s) - antagonist , metabolite , pharmacology , beta adrenoceptor , adrenergic beta antagonists , chemistry , sympathomimetics , adrenergic receptor , beta (programming language) , medicine , propranolol , receptor , computer science , programming language
We have tested the effects of carteolol and 8‐hydroxycarteolol on cAMP generation in S49 lymphoma and BC3H1 smooth muscle‐like cells. Carteolol was a high affinity beta‐adrenoceptor antagonist in both systems but did not stimulate cAMP accumulation. The metabolite 8‐ hydroxycarteolol also was a high affinity antagonist. In contrast to its parent compound, however, it possessed an agonistic component which was considerably stronger than that of other beta‐adrenoceptor blockers with intrinsic sympathomimetic activity, e.g. dichloroisoprenaline, pindolol, or celiprolol. These results suggest that metabolites can possess different pharmacodynamic properties in terms of beta‐ adrenoceptor interaction relative to parent compounds.