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.
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.
Korstanje
C
C
Sprenkels
R
R
Doods
H N
HN
Hugtenburg
J G
JG
Boddeke
E
E
Batink
H D
HD
Thoolen
M J
MJ
Van Zwieten
P A
PA
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D003655:Decerebrate State; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D007650:Ketanserin / Q000031:analogs & derivatives; D008297:Male; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D016713:Ritanserin; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013806:Theophylline / Q000031:analogs & derivatives / Q000494:pharmacology; D014661:Vasoconstriction / Q000187:drug effects
D000317:Adrenergic alpha-Antagonists; D006635:Histamine H2 Antagonists; D010880:Piperidines; D012702:Serotonin Antagonists; D016713:Ritanserin; C046301:seganserin; C049359:butanserin; C040397:fluprophylline; D007650:Ketanserin; D013806:Theophylline; C040398:flufylline