Table 2.
(A) Parameters of inhibition experiments with various reuptake inhibitor drugs on [3H]-5-hydroxytryptamine uptake into human and rat neocortical synaptosomes. (B) Parameters of inhibition experiments with various reuptake inhibitor drugs on [3H]-noradrenaline uptake into human and rat neocortical synaptosomes
| pIC50 | Imax | c | |
|---|---|---|---|
| A | |||
| Citalopram | |||
| Human | 8.44 (8.32, 8.56)*** | 0.88 (0.85, 0.92) | 1.04 (0.83, 1.35) |
| Rat | 8.78 (8.68, 8.88) | 0.97 (0.93, 1.01) | 1.21 (0.96, 1.57) |
| Fluvoxamine | |||
| Human§ | 7.96 (7.74, 8.15)** | 0.95 (0.89, 1.03) | 0.84 (0.60, 1.24) |
| Rat§ | 8.32 (8.21, 8.43) | 1.00 (0.97, 1.04) | 0.96 (0.798, 1.18) |
| Duloxetine | |||
| Human | 9.26 (9.09, 9.41)** | 0.95 (0.91, 1.00) | 0.43 (0.38, 0.50) |
| Rat | 8.81 (8.52, 9.04) | 1.05 (0.97, 1.15) | 0.44 (0.36, 0.54) |
| Fluoxetine | |||
| Human | 7.85 (6.57, 8.30) | 1.09 (0.91, 1.70) | 0.95 (0.28, −) |
| Rat | 7.48 (7.38, 7.58) | 1.00 (0.95, 1.08) | 1.01 (0.95, 1.08) |
| Milnacipran | |||
| Human | 7.80 (7.66, 7.93)*** | 0.93 (0.88, 0.99) | 0.95 (0.77, 1.20) |
| Rat | 7.39 (7.25, 7.53) | 1.01 (0.95, 1.07) | 0.79 (0.64, 1.00) |
| Atomoxetine | |||
| Human | 7.67 (7.51, 7.81)*** | 0.93 (0.88, 1.00) | 1.00 (0.74, 1.49) |
| Rat | 6.77 (6.65, 6.89) | 1.00 (0.94, 1.04) | 1.13 (0.88, 1.49) |
| Desipramine | |||
| Human | 7.16 (6.93, 7.34)*** | 0.96 (0.88, 1.06) | 0.80 (0.58, 1.12) |
| Rat | 5.97 (5.67, 6.11) | 1.02 (0.91, 1.27) | 1.19 (−, −) |
| (S,S)-Reboxetine | |||
| Human | 4.55 (4.18, 4.79)** | 1.11 (0.97, 1.38) | 0.88 (0.66, 1.24) |
| Rat | 5.08 (4.85, 5.21) | 0.89 (0.77, 1.12) | 1.35 (1.01, 1.77) |
| B | |||
| Citalopram | |||
| Human | 5.03 (2.57, 5.73) | 0.98 (0.68, 3.28) | 0.66 (0.34, 1.35) |
| Rat | 5.35 (5.21, 5.46) | 1.01 (0.94, 1.10) | 0.92 (0.75, 1.14) |
| Fluvoxamine | |||
| Human | 5.62 (5.29, 5.88)*** | 1.06 (0.94, 1.21) | 1.24 (0.75, 2.48) |
| Rat | 6.17 (6.07, 6.29) | 0.80 (0.73, 0.87) | 1.97 (1.42, 2.79) |
| Duloxetine | |||
| Human | 6.89 (5.44, 7.43) | 1.04 (0.80, 1.84) | 0.71 (0.34, 1.55) |
| Rat | 7.40 (7.26, 7.53) | 0.91 (0.86, 0.98) | 0.88 (0.70, 1.11) |
| Fluoxetine | |||
| Human | 5.94 (4.45, 7.14) | 0.90 (0.43, 3.09) | 0.66 (−, −) |
| Rat | 6.45 (6.07, 6.65) | 0.95 (0.83, 1.18) | 0.86 (0.57, 1.34) |
| Milnacipram | |||
| Human | 7.81 (7.31, 8.25) | 0.90 (0.71, 1.12) | 1.07 (0.58, 3.21) |
| Rat | 7.44 (7.31, 7.55) | 0.82 (0.78, 0.88) | 0.95 (0.77, 1.19) |
| Atomoxetine | |||
| Human | 9.51 (9.17, 9.83) | 0.92 (0.82, 1.03) | 0.83 (0.54, 1.39) |
| Rat | 9.58 (9.41, 9.74) | 0.90 (0.87, 0.94) | 0.55 (0.44, 0.71) |
| Desipramine | |||
| Human | 9.13 (8.83, 9.40) | 0.88 (0.77, 1.01) | 0.85 (0.58, 1.40) |
| Rat | 9.33 (9.11, 9.56) | 0.95 (0.89, 1.02) | 1.04 (0.65, 1.77) |
| (S,S)-Reboxetine | |||
| Human | 8.37 (7.89, 8.76)** | 0.87 (0.73, 1.05) | 0.96 (0.54, 2.04) |
| Rat | 8.98 (8.93, 9.04) | 0.75 (0.73, 0.77) | 1.83 (1.53, 2.27) |
Values given are estimates [CI95] (n≥ 2 independent experiments, at least six concentrations of drug/experiment, each concentration in six replicates).
A significant difference from the corresponding value for rat neocortex is indicated by asterisks
**
P≤ 0.01,
***
P≤ 0.001).
§
Data from Lieb et al. (2005).