Characterization of flufylline, fluprofylline, ritanserin, butanserin and R 56413 with respect to in‐vivo α1‐, α2‐ and 5‐HT2‐receptor antagonism and in‐vitro affinity for α1‐, α2‐ and 5‐HT2‐receptors: comparison with ketanserin

C. Korstanje, R. Sprenkels, H. N. Doods, J. G. Hugtenburg, E. Boddeke, H. D. Batink, M. J.M.C. Thoolen, P. A. Van Zwieten

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The experimental drugs butanserin (R 53393), ritanserin (R 55667), R 56413, flufylline (Sgd 195/78) and fluprofylline (Sgd 144/80) were evaluated with respect to their antagonism at postjunctional α1‐ and α2‐adrenoceptors and 5‐HT2‐receptors in pithed rats. Moreoever, affinity for [3H]mianserin, [3H]prazosin and [3H]yohimbine binding sites was assessed using rat brain preparations. In all experiments ketanserin was taken as a reference compound. It is concluded that of the compounds investigated butanserin is the most potent and selective α1‐adrenoceptor antagonist, whereas ritanserin was found to be a potent and selective 5‐HT2‐antagonist. Of the other compounds, fluprofylline was a very selective though not very potent α1‐adrenoceptor antagonist. The other compounds were less active and less selective in this respect.

Original languageEnglish
Pages (from-to)374-379
Number of pages6
JournalJournal of Pharmacy and Pharmacology
Issue number5
Publication statusPublished - 1 Jan 1986

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