Table 1.
Potencies to activate TAAR1
| No | Compound Name | EC50 (μM) | |
|---|---|---|---|
| Human | Rhesus | ||
| (S)-l | (S)-amphetamine | 0.6 ± 0.002 | 1.01 ± 0.08 |
| (R)-1 | (R)-amphetamine | 1.3 ± 0.03 | 1.86 ± 0.03 |
| (S)-2 | (S)-p-hydroxyamphetamine | 2.96 ± 0.1 | 0.101 ± 0.02 |
| (R)-2 | (R)-p-hydroxyamphetamine | 3.16 ± 1.2 | 0.424 ± 0.2 |
| (S)-3 | (S)-3,4-methylenedioxyamphetamine | 6.57 ± 1.2 | 1.35 ± 0.3 |
| (R)-3 | (R)-3,4-methylenedioxyamphetamine | 11.73 ± 6.3 | 2.48 ± 0.5 |
| (S)-4 | (S)-3,4-methylenedioxymethamphetamine | 73.7 ± 31 | 16.1 ± 6.8 |
| (R)-4 | (R)-3,4-methylenedioxymethamphetamine | inactive | 7.4 ± 0.5 |
| (S)-5 | (S)-m-methoxyamphetamine | 1.9 ± 0.9 | 3.3 ± 1.8 |
| (R)-5 | (R)-m-methoxyamphetamine | 6.5 ± 4.5 | inactive |
| (S)-6 | (S)-norfenfluramine | active* | ND |
| (R)-6 | (R)-norfenfluramine | inactive | ND |
| (S)-7 | (S)-4-bromo-2,5-dimethoxyamphetamine | 15.34 ± 0.1 | 2.14 ± 0.08 |
| (R)-7 | (R)-4-bromo-2,5-dimethoxyamphetamine | 31.94 ± 6.6 | 13.9 ± 5 |
| (S)-8 | (S)-4-methyl-2,5-dimethoxyamphetamine | inactive | 0.9 ± 0.04 |
| (R)-8 | (R)-4-methyl-2,5-dimethoxyamphetamine | inactive | inactive |
| (S)-9 | (S)-4-ethyl-2,5-dimethoxyamphetamine | 5.02 ± 1.8 | inactive |
| (R)-9 | (R)-4-ethyl-2,5-dimethoxyamphetamine | inactive | inactive |
| (S)-10 | (S)-methamphetamine | 1.5 ± 0.4 | 5.3 ± 0.5 |
| (R)-10 | (R)-methamphetamine | 3.3 ± 1.7 | 2.5 ± 1.2 |
ND= not determined
*
43% of maximum in screen, using 10 μM in hTAAR1/G 16 CHO-K1 cells loaded with Calcium 4 dye and analyzed using a FlexStation 2 microplate reader (Molecular Devices).