Influence of MCI-9042, a novel 5-HT2 receptor blocker on blood vessels of the rat.
We demonstrated that MCI-9042 potently inhibited the vasoconstrictory effects of serotonin in the isolated perfused hindlegs of the rat. Concentrations of MCI-9042 in the range of 0.01-1 mumol/l caused a dose-dependent inhibition of the vasoconstrictory effect of serotonin (1-30 micrograms/0.1 ml). The maximal inhibitory effect of MCI-9042 was about 97% (1 mumol/l). MCI-9042 caused a concentration-dependent shift to the right of concentration-response curve to serotonin in the rat tail artery. The present data demonstrate MCI-9042 as a potent 5-HT2 receptor antagonist.
Pawlak
D
D
Department of Pharmacodynamics, Medical Academy, Białystok, Poland.
Małyszko
J
J
Myśliwiec
M
M
Takada
A
A
Buczko
W
W
D000818:Animals; D001158:Arteries / Q000187:drug effects; D001808:Blood Vessels / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D006614:Hindlimb / Q000098:blood supply; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012701:Serotonin / Q000494:pharmacology; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013386:Succinates / Q000494:pharmacology*; D013623:Tail / Q000098:blood supply; D014661:Vasoconstriction / Q000187:drug effects
D012702:Serotonin Antagonists; D013386:Succinates; C064294:sarpogrelate; D012701:Serotonin