17a
Table 5. IC50 Values for Bupropion,
306U73, and 494U73 as inhibitors of 3H-Biogenic
Amine Uptake into
Synaptosomal Preparations of Various Rat and Mouse Brain
Areas.
|
|
IC50 Values (mean ±SE)a |
|
|
|
|
|
|
|
|
|
|
|
Hypothalamus |
|
Striatum |
|
|
|
3H-δ-NE |
3H-5HT |
|
3H-DA |
Compound |
Species |
(μM) |
(μM) |
|
(μM) |
Bupropion |
Rat |
5 ± 1.3 |
58 ± 15 |
|
2 ± 0.58 |
|
Mouse |
4.4 ± 0.75 |
36 ± 21 |
|
2.5 ± 0.82 |
|
|
|
|
|
|
306U73 |
Rat |
6.6 ± 3.3 |
105 ± 11 |
|
23 ± 8.3 |
|
Mouse |
3.6 ± 1.2 |
100 ± 11 |
|
17 ± 9 |
|
|
|
|
|
|
494U73 |
Rat |
16 ± 7.2 |
67 ± 2.1 |
|
47 ± 2.2 |
|
Mouse |
10 ± 13 |
92 ± 15 |
|
23 ± 13 |
|
|
|
|
|
|
Imipramine |
Rat |
.32 ± .11 |
.5 ± .04 |
|
58 ± 12 |
|
Mouse |
.10 ± .03 |
.45 ± .24 |
|
56 ± 11 |
|
|
|
|
|
|
aDrugs
were incubated in presence of the tissue for 5 minutes at 37˚ C before the
addition of 1x10-7M3H-1-NE, 1x10-7M3H-DM
or 1x10-7M3H-5HT.
Incubation was continued for an additional 5 minutes at 37˚ C in an
atmosphere of 95% 02 - 5%CO2. A minimum of 3 and in most cases 5 different
concentrations of the drug producing 30% - 70% inhibition of uptake of the
biogenic amines were used to determine the IC50 values. The results were plotted on
semilogarithmic paper. |
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