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.

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.

Publication types

  • Comparative Study

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology*
  • Animals
  • Binding, Competitive / drug effects
  • Blood Pressure / drug effects
  • Brain / metabolism
  • Decerebrate State
  • Histamine H2 Antagonists / pharmacology*
  • Ketanserin
  • Male
  • Piperidines / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Ritanserin
  • Serotonin Antagonists / pharmacology*
  • Theophylline / analogs & derivatives
  • Theophylline / pharmacology
  • Vasoconstriction / drug effects

Substances

  • Adrenergic alpha-Antagonists
  • Histamine H2 Antagonists
  • Piperidines
  • Serotonin Antagonists
  • Ritanserin
  • seganserin
  • butanserin
  • fluprophylline
  • Ketanserin
  • Theophylline
  • flufylline