Comparison of the densities of 5-HT4 receptors, beta 1- and beta 2-adrenoceptors in human atrium: functional implications.

We measured in human atrium the density of 5-HT4 receptors, labelled with [125I]-SB 207710 (1-butyl-4-piperidinyl) methyl 8-amino-7-iodo-1, 4-benzodioxan-5-carboxylate), and compared it with the density of beta1- and beta2-adrenoceptors, labelled with (-)-[125I]-cyanopindolol. [125I]-SB 207710 (5-1200 pmol/l) labelled a small population of saturable binding sites (Bmax approximately 4 fmol/mg protein) with a pK(D) of 9.7 and with 5-HT4 receptor characteristics, as assessed with competing ligands. The density of atrial binding sites with 5-HT4 receptor characteristics was 10 and 5 times lower, respectively, than the density of beta 1- and beta 2-adrenoceptors. We suggest that the small 5-HT4 receptor population may in part explain why the positive inotropic effects of 5-HT are smaller than those of catecholamines mediated through beta 1- and beta 2-adrenoceptors.