. 2021 Apr 13;11(4):570. doi: 10.3390/biom11040570

Table 1.

Pharmacological comparison of bitopic ligands at D3R.

D₃R, 10 min	Go Protein Activation Assay				β-arrestin Recruitment
Compounds	E_max ± SEM (% of Quinpirole)	pEC₅₀ ± SEM	Change E_max over Quinpirole	Fold Potency over Quinpirole	E_max ± SEM (% of Quinpirole)	pEC₅₀ ± SEM	Change E_max over Quinpirole	Fold Potency over Quinpirole
Quinpirole	100 ± 2.27 ^δδδδ	8.53 ± 0.08 ^δδδδ	0	1.000	100 ± 2.6 ^δδδδ	8.36 ± 0.09 ^δδδδ	0	1.000
rac-FOB02-04	74.4 ± 3.4 ***	7.67 ± 0.16 ***,^δδδδ	−25.6	0.138	68.5 ± 1.8 ***	6.78 ± 0.07 ****, ^δδδ	−31.5	0.026
FOB02-04A	82.8 ± 3.0 **^,δδ	8.22 ± 0.12 ^δδδδ	−17.2	0.490	80.2 ± 3.3 *	6.80 ± 0.10 ****, ^δδδδ	−19.8	0.028
FOB02-04B	78.4 ± 3.2 ****^,δδ	7.25 ± 0.11 ****, ^δδδδ	−21.6	0.052	112 ± 7.0 ^δδδδ	5.87 ± 0.10 ****	33.2	0.003
AB04-87	60.3 ± 8.1 ****	6.00 ± 0.23 ****	−39.7	0.003	67.2 ± 8.2 ****	5.80 ± 0.19 ****	−32.8	0.003
AB04-88	111.6 ± 2.8 ^δδδδ	9.34 ± 0.09 ***,^δδδδ	11.6	6.500	110 ± 0.9 ^δδδδ	7.03 ± 0.10 ****, ^δδδδ	10.0	0.047
rac-AB04-35	93.9 ± 3.0 ^δδδδ	7.24 ± 0.07 ****, ^δδδδ	−6.1	0.051	94.8 ± 3.7 ^δδ	6.31 ± 0.07 ****, ^δ	−5.2	0.009
AB04-95	ND	ND	ND	ND	ND	ND	ND	ND
AB04-96	100.4 ± 2.7 ^δδδδ	7.73 ± 0.08 ***, ^δδδδ	0.4	0.158	104.0 ± 2.9 ^δδδ	6.76 ± 0.06 ****, ^δδδ	4.0	0.025

Mean E_max ± SEM and pEC50 ± SEM values along with fold changes over the reference D2R and D3R agonist—quinpirole are reported. Using Dunnett’s multiple comparisons tests, statistical significance are reported as ‘*’ representing significance of p < 0.05; ‘**’ of p < 0.01; ‘***’ of p < 0.001 and ‘****’ of p < 0.0001 compared to quinpirole, and ‘^δ’ of p < 0.05; ‘^δδ’ of p < 0.01; ‘^δδδ’ of p < 0.001 and ‘^δδδδ’ of p < 0.0001 compared to AB04-87. ND, not determined.