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Derivatives of Compound 1 as modulators of hGAT1.
 | |||||
|---|---|---|---|---|---|
| Compound 1 | |||||
| Bridging cell represented by “A” | r | s | R | GABA uptake IC50 (μM) | |
| Compound 1 | CH2CH2 | 2 | 2 | homo-β-proline (HOM) | 0.05 |
| Derivatives of Compound 1 | CH2CH2 | 2 | 2 | (R)-nipecotic acid | 0.18 |
| S | 2 | 2 | (R)-nipecotic acid | 0.30 | |
| O | 2 | 2 | (R)-nipecotic acid | 14.6 | |
| CH2 | – | – | (R)-nipecotic acid | >40 | |
