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

Publisher Website
Google Scholar
Abstract
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.

This publication has 25 references indexed in Scilit: