1. Academic Validation
  2. Characterization of flufylline, fluprofylline, ritanserin, butanserin and R 56413 with respect to in-vivo alpha 1-,alpha 2- and 5-HT2-receptor antagonism and in-vitro affinity for alpha 1-,alpha 2- and 5-HT2-receptors: comparison with ketanserin

Characterization of flufylline, fluprofylline, ritanserin, butanserin and R 56413 with respect to in-vivo alpha 1-,alpha 2- and 5-HT2-receptor antagonism and in-vitro affinity for alpha 1-,alpha 2- and 5-HT2-receptors: comparison with ketanserin

  • J Pharm Pharmacol. 1986 May;38(5):374-9. doi: 10.1111/j.2042-7158.1986.tb04590.x.
C Korstanje R Sprenkels H N Doods J G Hugtenburg E Boddeke H D Batink M J Thoolen P A Van Zwieten
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 alpha 1- and alpha 2-adrenoceptors and 5-HT2-receptors in pithed rats. Moreover, 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 alpha 1-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 alpha 1-adrenoceptor antagonist. The other compounds were less active and less selective in this respect.

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