. 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 1.

Human D₂-like receptor binding data for synthons^a


Compd.	R	A	B	C	D₂R	D₃R	D₄R	D₂/D₃	D₄/D₃	D₄/D₂

					K_i±S.E.M. (nM)
11a	H	H	OMe	Cl	619±97.6	446±25.2	2300±820	1.4	5.2	3.7
11b	H	Cl	H	H	139±11.9	31.1±0.462	316±47.1	4.5	10	2.3
12a	Me	H	OMe	Cl	233±22.4	179±18.1	400±83.4	1.3	2.2	1.7
12b	Me	Cl	H	H	58.1±3.09	13.6±0.488	89.9±6.81	4.3	6.6	1.5
13a	n-But	H	OMe	Cl	29.8±4.58	22.5±4.86	322±76.0	1.3	14	11
13b	n-But	Cl	H	H	2.93±0.316	0.363±0.052	65.1±10.0	8.1	179	22

Binding inhibition values determined using HEK 293 cells transfected with hD_2LR, hD₃R or hD_4.4 and [³H]N-methylspiperone radioligand as described.⁵⁹