Comparison between ketanserin and LY 53857 on vascular and cardiac 5-HT2 and alpha 1-adrenergic receptors in the pithed rat.
In normotensive pithed rats, both ketanserin and LY 53857 potently antagonized the increase in blood pressure induced by 5-HT in a noncompetitive manner. However, LY 53857 differs from ketanserin in that it shifts the pressor dose-response curve to 5-HT in a parallel way at low doses but in a noncompetitive way at higher doses. Ketanserin and LY 53857 were weak antagonists of the pressor effects of phenylephrine. LY 53857 was more potent and more selective than ketanserin for 5-HT2 vs alpha 1-adrenergic receptors.
Dabiré
H
H
INSERM U 228, Faculté de Médecine Broussais Hôtel-Dieu, Paris, France.
Chaouche-Teyara
K
K
Cherqui
C
C
Fournier
B
B
Schmitt
H
H
D000317:Adrenergic alpha-Antagonists; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D003655:Decerebrate State; D004305:Dose-Response Relationship, Drug; D004873:Ergolines / Q000494:pharmacology*; D006321:Heart / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D007650:Ketanserin / Q000494:pharmacology*; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000378:metabolism*; D009206:Myocardium / Q000378:metabolism*; D010656:Phenylephrine / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000494:pharmacology*
D000317:Adrenergic alpha-Antagonists; D004873:Ergolines; D011942:Receptors, Adrenergic, alpha; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D010656:Phenylephrine; D007650:Ketanserin; C032663:LY 53857