Table 1

Comparison of the KI values of 5 psychostimulants to inhibit human and mouse monoamine transporters.

Drug

Cocaine

Methylphenidate

Amphetamine

Methamphetamine

MDMA


Human

hDAT

0.23 ± 0.03

0.06 ± 0.01

0.64 ± 0.14

0.46 ± 0.06

8.29 ± 1.67

hNET

0.48 ± 0.05

0.10 ± 0.01

0.07 ± 0.01

0.11 ± 0.01

1.19 ± 0.13

hSERT

0.74 ± 0.03

132.43 ± 10.71

38.46 ± 3.84

31.74 ± 2.40

2.41 ± 0.73

Ratio 1

3.2

2207

549

288

7.0

Mouse

mDAT

0.49 ± 0.04 2

0.26 ± 0.03

0.56 ± 0.11

0.47 ± 0.08

4.87 ± 0.65

mNET

0.46 ± 0.06 2

0.17 ± 0.03

0.12 ± 0.02

0.19 ± 0.05

1.75 ± 0.51

mSERT

0.73 ± 0.12

114.37 ± 7.61

23.82 ± 1.71

9.28 ± 0.86

0.64 ± 0.05

Ratio 1

1.6

672

199

49

7.6


The KI values (in μM) were determined as illustrated in Fig. 1. They are expressed as mean ± S.E.M. of four to seven experiments. 1 The ratios of highest KI values over the lowest are shown to highlight the differences. 2 The difference between these two KI values was not statistically significant (ANOVA post hoc Bonferroni test, p > 0.05); all other values were statistically different (ANOVA comparing the three transporters within the same species and for the same drug).

Han and Gu BMC Pharmacology 2006 6:6   doi:10.1186/1471-2210-6-6

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