Table 1.
Summary of Serotonergic and Dopaminergic Effects of Selected Releasing Agents
| Drug | [3H]5-HT release EC50 (nM) | [3H]DA release EC50 (nM) | Peak % increase in dialysate 5-HT (dose, mg/kg) | Peak % increase in dialysate DA (dose, mg/kg) | Self- administered | Locomotor activation |
|---|---|---|---|---|---|---|
| Amphetaminea | 1756 | 8.0 | 45 (0.3 mg/kg ip) | 224 (0.3 mg/kg ip) | Yes | Strong |
| Phenterminea | 3511 | 262 | 32 (1.0 mg/kg ip) | 156 (1.0 mg/kg ip) | Yes | Strong |
| PAL-353b | 1937 | 24.2 | 170 (1.0 mg/kg iv) | 432 (1.0 mg/kg iv) | Yes | Strong |
| Fenfluraminea | 79.3 | >10,000 | 215 (1.0 mg/kg ip) | 20 (1.0 mg/kg ip) | No | None |
| Chlorphenterminea | 30.9 | 2650 | 228 (1.0 mg/kg ip) | 86 (1.0 mg/kg ip) | No | None |
| Phentermine + fenfluraminea | NA | NA | 222 (1.0 + 1.0 mg/kg, ip) | 144 (1.0 + 1.0 mg/kg ip) | No | Weak |
| PAL-313b | 53.4 | 44.1 | 544 (1.0 mg/kg iv) | 130 (1.0 mg/kg iv) | Weak | Weak |
| PAL-287c | 3.4 | 12.6 | 464 (1.0 mg/kg iv) | 133 (1.0 mg/kg iv) | No | Weak |
Note. 5-HT = serotonin; EC50 = half maximal effective concentration; DA = dopamine; NA = not applicable. A summary of data illustrating the tendency for increasing extracellular 5-HT to reduce reinforcing and locomotor effects mediated by increases in extracellular DA.
a
From Baumann et al. (2000) and Rothman et al. (2001).
b
From Wee et al. (2005). Microdialysis data unpublished. This table originally appeared in Rothman, Blough, and Baumann (2007).
c
From Rothman et al. (2005).