Table 3.
Examples of monoamine transporter affinity and inhibition for 2C and NBOMe drugs.
|
Drug / Transporter |
DAT | NET | SERT | Model | Ref |
|---|---|---|---|---|---|
|
Transporter Binding Ki (nM) |
|||||
| 2C-D | > 10,000 | > 8500 | > 10,000 | HEK293 cells expressing human DAT, NET or SERT | [29] |
| 2C-E | > 10,000 | > 7600 | > 10,000 | ||
| 2C-I | > 1,0000 | > 10,000 | 950 | ||
| 25D-NBOMe | 34,500 | 6700 | 1780 | [24] | |
| 25E-NBOMe | 19,600 | 5400 | 1590 | ||
| 2C-B | > 30,000 | 31,000 | 9700 | [25] | |
| 25B-NBOMe | 7200 | 1100 | 840 | ||
| 2C-I | > 30,000 | 15,000 | 4900 | ||
| 25I-NBOMe | 5400 | 1300 | 1000 | ||
| 2C‐T‐4 | > 8710 | > 9710 | > 8580 | [27] | |
| 2C‐T‐7 | > 8710 | > 9710 | > 8580 | ||
|
Inhibition potency IC50 (nM) |
|||||
| 2C-D | > 10,000 | > 9200 | > 8400 | HEK293 cells expressing human DAT, NET or SERT | [29] |
| 2C-E | > 10,000 | > 9800 | > 7500 | ||
| 2C-I | > 9600 | > 8200 | 5600 | ||
| 25D-NBOMe | > 85,000 | 1170 | 1024 | [24] | |
| 25E-NBOMe | 34,000 | 2310 | 1440 | ||
| 2C-B | 231,000 | 44,000 | 18,000 | [25] | |
| 25B-NBOMe | 117,000 | 6700 | 7100 | ||
| 2C-I | 126,000 | 22,000 | 13,000 | ||
| 25I-NBOMe | 65,000 | 10,000 | 6800 | ||
| Methylphenidate | 120 | - | - | ||
| Reboxetine | - | 36 | - | ||
| Citalopram | - | - | 45 | ||
| 2C-B | 132,000 | 122,000 | 4700 | [34] | |
| 25B-NBOMe | 99,000 | 11,000 | 4900 | ||
| 25I-NBOMe | 53,000 | 11,000 | 4000 | ||
| Cocaine | 1000 | 1100 | 1400 | ||
| Methoxetamine | 24,000 | 15,000 | 2400 | ||