Comparison of the effect of irindalone, a novel serotonin 5-HT2 antagonist and ketanserin on mechanical responses of rat thoracic aorta.
The relaxant effect of irindalone [+)-(1R, 3.S)-1-[2-[4-[3-(p-fluorophenyl)-1-indanyl]-1-piperazinyl] ethyl]2-imidazolidinone) and ketanserin was studies on active tension in isolated rat thoracic aorta. Irindalone and ketanserin caused a concentration-related inhibition of serotonin-induced contractions and shifted the serotonin curve to the right. Irindalone was more potent in inhibiting the serotonin-induced contractions and ketanserin was. The slopes of the Schild plots for the two substances were slightly, but not significantly, different from each other. This indicates that irindalone had a more pronounced serotonin antagonistic effect than ketanserin.
Mikkelsen
E O
EO
Institute of Pharmacology, University of Aarhus, Denmark.
Nyborg
N C
NC
Jensen
K T
KT
Boeck
V
V
D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D007093:Imidazoles / Q000494:pharmacology*; D066298:In Vitro Techniques; D007650:Ketanserin / Q000494:pharmacology*; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D010879:Piperazines; D051381:Rats; D011919:Rats, Inbred Strains; D012702:Serotonin Antagonists / Q000494:pharmacology*
D007093:Imidazoles; D010879:Piperazines; D012702:Serotonin Antagonists; C056634:irindalone; D007650:Ketanserin