Table 2.

Receptor activation profile of ADN-1184

Receptor	Functional test	Agonist	Kb ± SEM
h 5-HT6	cAMP	5-HT (300 nM)	24 ± 13
h 5-HT7	cAMP	5-HT (300 nM)	0.11 ± 0.04
h 5-HT2A	IP1	5-HT (100 nM)	3.4 ± 1.0
h 5-HT1A	Cellular dielectric spectroscopy	8-OH-DPAT (100 nM)	116 ± 43
h 5-HT2C	IP1	5-HT (10 nM)	>1000
h D2S	cAMP	Dopamine (300 nM)	2.4 ± 1.1
h D3	cAMP	Dopamine (10 nM)	3.9 ± 1.1
h D4	cAMP	Dopamine (100 nM)	22 ± 4
h D1	cAMP	Dopamine (300 nM)	140 ± 10a
h α1A	Intracellular Ca2+ release	Adrenaline (3 nM)	0.16 ± 0.07

When tested alone, ADN-1184 did not show agonist properties in any of the assays. The cell lines used are the same as those shown in Table 2009. Experiments were carried out by Cerep. For further methodological information, see the company's online catalogue (http://www.cerep.fr). K_B values of antagonists for inhibition of agonist action were calculated according to Lazareno and Birdsall (1993): [K_B = IC₅₀: 1 + (Agonist/EC₅₀)], where IC₅₀ = inhibitory concentration₅₀ of antagonist, agonist = concentration of agonist in the test, and EC₅₀ = effective concentration₅₀ of agonist.

^aMean ± range.

h, human recombinant; IP1, inositol phosphate.