Blockade of human atrial 5-HT4 receptors by SB 207710, a selective and high affinity 5-HT4 receptor antagonist.
The mode of antagonism of 5-hydroxytryptamine-induced positive inotropic effects by the highly selective 5-HT4 receptor antagonist SB 207710 (1-butyl-4-piperidinyl) methyl 8-amino-7-iodo-1,4-benzodioxan-5-carboxylate) was investigated on isolated preparations of human right atrial appendage. SB 207710 caused concentration-dependent (0.1-10 nmol/l) surmountable antagonism of the effects of 5-hydroxytryptamine with a pKB (mol/l) of 10.1. Due to its high selectivity and affinity, SB 207710 could be a powerful tool for the comparison of human atrial 5-HT4 receptors with 5-HT4 receptors of other organs of man and other species.
Kaumann
A J
AJ
Clinical Pharmacology Unit, University of Cambridge, Addenbrooke's Hospital, UK.
Gaster
L M
LM
King
F D
FD
Brown
A M
AM
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000368:Aged; D000369:Aged, 80 and over; D004146:Dioxanes / Q000494:pharmacology*; D005260:Female; D006325:Heart Atria / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology; D008297:Male; D008875:Middle Aged; D009200:Myocardial Contraction / Q000187:drug effects*; D010880:Piperidines / Q000494:pharmacology*; D012701:Serotonin / Q000494:pharmacology; D012702:Serotonin Antagonists
D000319:Adrenergic beta-Antagonists; D004146:Dioxanes; D007093:Imidazoles; D010880:Piperidines; C088873:SB 207710; D012702:Serotonin Antagonists; D012701:Serotonin; C049763:CGP 20712A