. 2011 Feb;336(2):575–585. doi: 10.1124/jpet.110.173260

TABLE 2.

Affinities of N-substituted BZT analogs in binding to the transporters for dopamine, norepinephrine, and serotonin, and M₁ muscarinic, histamine H₁, σ₁, and σ₂ receptors

Numbers are K_i values in nM with S.E.M. or 95% confidence limits.

Target	GA 1-69	GA 2-50	GA 2-99	JHW 013
DAT	29.2 ± 3.24	13.2 ± 1.50	5.59 ± 0.619	24.6 ± 1.70
SERT	490 ± 56.4	3870 ± 135	4600 ± 680	1420 ± 116
NET	7350 ± 934	2130 ± 160	1420^a ± 125	1640 ± 153
M₁	3280 ± 221^b	4020 ± 592^b	1250 ± 138^b	257 ± 28.9^b
H₁	333 ± 22.6^c	218 ± 15.5^c	240 ± 32.6^c	48.3 ± 5.54
σ₁	430 (385–479)	12.1 (10.9–13.5)	129 (110–150)	6.90 (6.31–7.57)
σ₂	65.8 (50.8–85.1)^d	18.1 (15.0–21.8)^d	156 (111–219)^d	25.9 (20.0–33.8)^d

SERT, serotonin transporter; NET, norepinephrine transporter.

Data were published in Kulkarni et al., 2004.

Data were published in Robarge et al., 2000.

Data were published in Campbell et al., 2005.

The K_i values reported are from a [³H]DTG binding assay in which the data uniformly modeled better for two than one binding site. The K_i value for the higher affinity site is displayed. The obtained high-affinity site is the site recognized as the σ₂ receptor, whereas the low-affinity site is currently not identified. Values for the low-affinity DTG site and their 95% confidence limits were as follows: GA 1-69, 14,600 (3860–55,000); GA 2-50, 6500 (2830–14,900); GA 2-99, 8490 (424–171,000); JHW 013, 12,100 (4280–34,000).