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 Ki 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 | 1420a ± 125 | 1640 ± 153 |
| M1 | 3280 ± 221b | 4020 ± 592b | 1250 ± 138b | 257 ± 28.9b |
| H1 | 333 ± 22.6c | 218 ± 15.5c | 240 ± 32.6c | 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.
↵a Data were published in Kulkarni et al., 2004.
↵b Data were published in Robarge et al., 2000.
↵c Data were published in Campbell et al., 2005.
↵d The Ki values reported are from a [3H]DTG binding assay in which the data uniformly modeled better for two than one binding site. The Ki 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).