Table 3.
Ki (nM) |
||||||||
---|---|---|---|---|---|---|---|---|
Compound | R1 | R2 | R3 | SERT | DAT | NET | Ref. | |
41 | ADAM | I | H | H | 0.013 | 840 | 699 | [209] |
42 | DASB | CN | H | H | 1.10 | 1423 | 1350 | [211] |
43 | DAPP | OMe | H | H | 1.89 | 2651 | 1992 | [211] |
44 | DAPA | Br | H | H | 0.38 | N/A | N/A | [213] |
45 | HOMADAM | CH2OH | H | H | 0.57 | >1000 | 144 | [218] |
46 | EADAM | Et | H | H | 0.17 | >1000 | 367 | [217] |
47 | AFA, | F | H | H | 1.46 | >10,000 | 141.7 | [215] |
4-F-ADAM | F | H | H | 0.08 | 2267 | 117 | [222] | |
48 | CF3 | H | H | 0.33 | 2038 | 1205 | [211] | |
49 | AFM | CH2F | H | H | 1.04 | >10,000 | 664 | [214] |
50 | AFE | CH2CH2F | H | H | 1.80 | >10,000 | 946 | [216] |
51 | AFP | CH2CH2CH2F | H | H | 3.58 | >10,000 | 505 | [223] |
52 | 5-F-ADAM | H | F | H | 0.47 | N/A | N/A | [224] |
53 | ACF | Cl | F | H | 0.05 | 3020 | 650 | [225] |
54 | H | H | OCH2CH2F | 0.25 | 340 | 7.5 | [226] | |
55 | F | H | OCH2CH2F | 0.10 | >1000 | 37 | [226] | |
56 | Cl | H | OCH2CH2F | 0.03 | 847 | 97 | [226] | |
57 | Br | H | OCH2CH2F | 0.05 | >1000 | 114 | [226] | |
58 | H | H | OCH2CH2CH2F | 1.4 | 299 | 12 | [226] | |
59 | F | H | OCH2CH2CH2F | 0.95 | >1000 | 95 | [226] | |
60 | Br | H | OCH2CH2CH2F | 0.15 | >1000 | >1000 | [226] | |
61 | CH2OH | H | F | 1.26 | >2000 | 618 | [227] |