. Author manuscript; available in PMC: 2017 Aug 25.

Published in final edited form as: J Med Chem. 2016 Aug 10;59(16):7634–7650. doi: 10.1021/acs.jmedchem.6b00860

Table 4.

Additional in vitro binding and functional data for selected compounds at 5HT_1A, 5HT_2A and 5HT_2C receptors^a

Compd	5-HT_1A [³H]-8-OH-DPAT K_i ± SEM, nM	5-HT_2A [¹²⁵I]DOI K_i ± SEM, nM	5-HT_2C [¹²⁵I]DOI K_i ± SEM, nM	5HT_1A [³⁵S]GTPγS binding
Compd	5-HT_1A [³H]-8-OH-DPAT K_i ± SEM, nM	5-HT_2A [¹²⁵I]DOI K_i ± SEM, nM	5-HT_2C [¹²⁵I]DOI K_i ± SEM, nM	Agonist EC₅₀ ± SEM, nM	% Stimulation
11a	3560 ± 490	90.4 ± 4.7	22.4 ± 1.9	ND^b	-
11b	70.3 ± 4.2	7.00 ± 2.1	5.40 ± 1.6	77.0 ± 23	90.1
12a	4400 ± 1000	140 ± 14	17.2 ± 5.3	ND^b	-
12b	40.3 ± 8.9	3.22 ± 0.93	4.00 ± 1.3	27.7 ± 8.3	89
13a	2260 ± 490	470 ± 130	1000 ± 190	ND^b	-
13b	37.0 ± 8.9	53.0 ± 15	222 ± 59	48.0 ± 13	90.8
18	2330 ± 700	60.1 ± 9.5	144 ± 37	ND^b	-
19	>7600	188 ± 22	2190 ± 460	ND^b	-
20	560 ± 170	25.0 ± 6.6	55.0 ± 17	ND^b	-
21	2410 ± 830	42.9 ± 6.8	268 ± 34	ND^b	-
22	59 ± 13	5.22 ± 0.98	18.3 ± 2.2	149 ± 47	94.3
23	880 ± 160	28.1 ± 9.7	113 ± 33	ND^b	-
24	26.0 ± 8.1	2.41 ± 0.82	18.7 ± 4.5	31.0 ± 10	99.4
25	27.6 ± 5.3	3.20 ± 1.1	89.0 ± 22	118 ± 39	101.1

Data were obtained through the NIDA Addiction Treatment Discovery Program contract (ADA151001) with Oregon Health & Science University.

ND = Not determined; Functional assays for each receptor was not conducted if the K_i value for the binding assay was >250 nM for 5-HT receptors.