Table 1.

Receptor binding profile of ADN-1184

Receptor	Cell line	Radioligand or readout	Reference ligand (Ki, nM)	ADN-1184 Ki ± SEM (nM)
h 5-HT6	CHO cells	[3H]LSD	5-HT (33)	16 ± 13
h 5-HT7	CHO cells	[3H]LSD	5-HT (0.8)	0.50 ± 0.27
h 5-HT2A	HEK-293 cells	[3H]ketanserin	Ketanserin (0.3)	2.0 ± 1.0
h 5-HT1A	HEK-293 cells	[3H]8-OH-DPAT	8-OH-DPAT (0.4)	173 ± 85
h 5-HT2C	HEK-293 cells	[3H]mesulergine	RS102221 (0.6)	630 ± 370
h D2S	HEK-293 cells	[3H]methyl-spiperone	(+)butaclamol (0.04)	18 ± 6
h D3	CHO cells	[3H]methyl-spiperone	(+)butaclamol (0.04)	20 ± 11
h D4	CHO cells	[3H]methyl-spiperone	Clozapine (17)	17 ± 7
h D1	CHO cells	[3H]SCH23390	SCH23390 (0.1)	30 ± 13
h α1A	CHO cells	[3H]prazosin	Prazosin (0.04)	0.84 ± 0.58
h α2C	CHO cells	[3H]RX 821002	Yohimbine (0.5)	8.5 ± 5.7
h H1	HEK-293 cells	[3H]pyrilamine	Pyrilamine (1.7)	116 ± 60
h M1	CHO cells	[3H]pirenzepine	Pirenzepine (16)	>1000a
h M2	CHO cells	[3H]AF-DX 384	Methoctramine (27)	>1000a
h M3	CHO cells	[3H]4-DAMP	4-DAMP (0.44)	>1000a
h M4	CHO cells	[3H]4-DAMP	4-DAMP (0.88)	>1000a
h M5	CHO cells	[3H]4-DAMP	4-DAMP (0.48)	>1000a
hERG	CHO cells	Inhibition of K + current	–	2080 ± 550b

Unless indicated, all experiments were carried out by Cerep.

^aLess than 10% inhibition of binding observed at a concentration of 1 μM (n = 2).

^bIC₅₀ value. hERG channel current experiments were carried out by ChanTest.

h, human recombinant.