Table 2. MAT Binding Data for Thio- and Sulfinylethanamine Analoguesa.
Ki [SE interval] (nM) |
||||||
---|---|---|---|---|---|---|
compd | X | Y | R | DAT | SERT | NET |
6a | H | S | H | 142 [131–155] | 221 [191–257] | 980 [938–1020] |
6b | Cl | S | H | 296 [272–323] | 29.8 [28.2–31.5] | 6920 [6340–7550] |
6c | Br | S | H | 483 [434–536] | 26.1 [23.9–28.5] | 8540 [7980–9130] |
6d | H | S | cyclopropylmethyl | 435 [406–466] | 10000 [9570–10400] | 17300 [15400–19400] |
6e | H | S | n-butyl | 310 [275–350] | 5700 [5040–6440] | 11500 [10700–12300] |
6f | H | S | 3-phenylpropyl | 295 [268–325] | 927 [786–1090] | 5500 [5140–5880] |
6g | F | S | 3-phenylpropyl | 114 [97.4–132] | 354 [312–402] | 3850 [3830–3870] |
6i | Br | S | 3-phenylpropyl | 613 [564–667] | 163 [156–170] | 3160 [2950–3390] |
7a | H | S=O | H | 1110 [1020–1200] | 3380 [2970–3820] | 24500 [22800–26200] |
7b | H | S=O | n-butyl | 1570 [1490–1660] | 63600 [56100–72200] | 138000 [103000–184000] |
7c | F | S=O | 3-phenylpropyl | 183 [140–239] | 1280 [1100–1480] | 3270 [3130–3420] |
7d | Cl | S=O | 3-phenylpropyl | 645 [565–736] | 553 [513–595] | 5670 [5000–6420] |
7e | Br | S=O | 3-phenylpropyl | 1270 [1130–1420] | 557 [493–628] | 8650 [7450–10000] |
2b | H | S=O | 3-phenylpropyl | 192 [177–209] | 987 [870–1120] | 2320 [2060–2620] |
Each Ki value represents data from at least three independent experiments, each performed in triplicate. Ki values were analyzed by PRISM. Binding assays are described in detail in the Experimental Methods.
Previously reported by Cao et al.10