Table 1: Binding profiles of the 5-HT7 receptor agonists AS-19, E-57431, and E-55888.

ReceptorAffinity (Ki (nM))
AS-19E-57431E-55888

h5-HT1A89.7 (149.5 x)n.s.700 (280 x)
r5-HT1B490 (816.6 x)n.s.n.s.
h5-HT1D6.6 (11 x)53 (112.7 x)n.s.
h5-HT2An.s.560 (1191.5 x)n.s.
h5-HT2Bn.s.n.s.n.s.
h5-HT2Cn.s.n.s.n.s.
h5-HT3n.s.n.s.n.s.
h5-HT4en.s.n.s.
gp5-HT4n.s.n.s.
h5-HT5A98.5 (164.2 x)n.s.n.s.
h5-HT6n.s.n.s.n.s.
h5-HT70.60.472.5
h5-HT transporter (SERT)n.s.n.s.n.s.
Other receptorsn.s.an.s.bn.s.a

n.s.: not significant (Ki > 1 μM or less than 50% inhibition of specific radioligand binding at 1 μM);
—: data not available.
gp: guinea pig; h: human; r: rat.
Data obtained from Brenchat et al. [13, 14]
Data in parentheses after Ki values represent the affinity ratio versus 5-HT7 receptors calculated as Ki for the tested receptor/Ki for 5-HT7 receptor. It is expressed as number-fold higher (x) for 5-HT7 than for the tested receptor.
aSee the panel of other receptors assayed [13].
bSee the panel of other receptors assayed [14].