Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs

BMC Pharmacology
Dawn D Han, Howard H Gu

Abstract

The plasma membrane neurotransmitter transporters terminate neurotransmissions by the reuptake of the released neurotransmitters. The transporters for the monoamines dopamine, norepinephrine, and serotonin (DAT, NET, and SERT) are targets for several popular psychostimulant drugs of abuse. The potencies of the psychostimulant on the monoamine transporters have been studied by several laboratories. However, there are significant discrepancies in the reported data with differences up to 60-fold. In addition, the drug potencies of the 3 monoamine transporters from mouse have not been compared in the same experiments or along side the human transporters. Further studies and systematic comparisons are needed. In this study, we compared the potencies of five psychostimulant drugs to inhibit human and mouse DAT, SERT and NET in the same cellular background. The KI values of cocaine to inhibit the 3 transporters are within a narrow range of 0.2 to 0.7 microM. In comparison, methylphenidate inhibited DAT and NET at around 0.1 microM, while it inhibited SERT at around 100 microM. The order of amphetamine potencies was NET (KI = 0.07-0.1 microM), DAT (KI approximately 0.6 microM), and SERT (KI between 20 to 40 microM). The results for met...Continue Reading

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Methods Mentioned

BETA
PCR

Software Mentioned

mNET
Origin
mSERT

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