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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