Table 2.

In vitro Binding of Amine-linked Analogs at D2R and D3R^a

compound	temp	R	Ar	R′	R″	D2R Ki ± S.E.M., nM	D3R Ki ± S.E.M., nM	D2/D3
13a	B	2-OCH3		H	n-propyl	69.9±7.3	67.9±2.4	1
13b	B	2,3-diCl		H	n-propyl	162.0±1.2	101±27	2
13c	B	2-OCH3		H	n-propyl	196±30	71.5±2.0	3
13d	B	2,3-diCl		H	n-propyl	269±24	129.±30	2
13e	B	2-OCH3		H	n-propyl	119 ± 11	80.8±32	1.5
13f	B	2,3-diCl		H	n-propyl	313 ± 8.4	104±21	3
14a	B	2,3-diCl		OH	H	2090 ± 370	134±23	16
14b	B	2,3-diCl		F	H	5270±1900	467±60	11
15a	B	2,3-diCl		OH	Me	869±140	162±32	5
15b	B	2,3-diCl		F	Me	2060±320	393±38	5
16e	A	2-OCH3		H	-	33.6±5.9	0.30±0.06	112
17b,f	A	2,3-diCl		H	-	112 ± 22	2.00±0.4	56
18c,g	A	2-OCH3		H	-	55.4±5.3	0.30±0.1	185
19b,h	A	2,3-diCl		H	-	64.7±8.9	0.80±0.2	81
20b,i	A	2,3-diCl		H	-	44.8±11	0.80±0.3	56

^aBinding inhibition values determined using HEK 293 cells transfected with hD2_LR or hD3R dopamine receptors and¹²⁵I-IABN radioligand as described.^5,6

^bdata previously reported in ref. 5;

^cdata previously reported in ref. 6.

^eBP 897 (N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-2-naphthamide);

^fNGB 2904 (N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide);

^gPG 576 (N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide);

^hPG01032 (Benzo[b]thiophene-2-carboxylic acid {4-[4-(2,3-dichloro-phenyl)-piperazin-1-yl]-butyl}-amide);

ⁱPG01059 (N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)benzofuran-2-carboxamide).