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.
|Number of pages||6|
|Journal||Journal of Pharmacy and Pharmacology|
|Publication status||Published - 1 Jan 1986|