Assessment of 5-HT₇ Receptor Agonists Selectivity Using Nociceptive and Thermoregulation Tests in Knockout versus Wild-Type Mice

Table 1

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

Receptor	Affinity (Ki (nM))
	AS-19	E-57431	E-55888
h5-HT1A	89.7 (149.5 x)	n.s.	700 (280 x)
r5-HT1B	490 (816.6 x)	n.s.	n.s.
h5-HT1D	6.6 (11 x)	53 (112.7 x)	n.s.
h5-HT2A	n.s.	560 (1191.5 x)	n.s.
h5-HT2B	n.s.	n.s.	n.s.
h5-HT2C	n.s.	n.s.	n.s.
h5-HT3	n.s.	n.s.	n.s.
h5-HT4e	—	n.s.	n.s.
gp5-HT4	n.s.	n.s.	—
h5-HT5A	98.5 (164.2 x)	n.s.	n.s.
h5-HT6	n.s.	n.s.	n.s.
h5-HT7	0.6	0.47	2.5
h5-HT transporter (SERT)	n.s.	n.s.	n.s.
Other receptors	n.s.^a	n.s.^b	n.s.^a

n.s.: not significant (K_i > 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 K_i values represent the affinity ratio versus 5-HT₇ receptors calculated as K_i for the tested receptor/K_i 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].