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Research ArticleCELLULAR AND MOLECULAR

Agmatine Is Efficiently Transported by Non-Neuronal Monoamine Transporters Extraneuronal Monoamine Transporter (EMT) and Organic Cation Transporter 2 (OCT2)

Dirk Gründemann, Christian Hahne, Reinhard Berkels and Edgar Schömig
Journal of Pharmacology and Experimental Therapeutics February 2003, 304 (2) 810-817; DOI: https://doi.org/10.1124/jpet.102.044404
Dirk Gründemann
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Christian Hahne
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Reinhard Berkels
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Edgar Schömig
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Abstract

Agmatine has received considerable attention recently. Available evidence suggests that agmatine functions as a neurotransmitter and inhibits, via induction of antizyme, cellular proliferation. Because of its positive charge, agmatine will not appreciably cross cellular membranes by simple diffusion. Indeed, all physiological models require a channel or transporter protein in the plasma membrane to effect inactivation or nonexocytotic release of agmatine. However, a transport mechanism for agmatine has not been identified on a molecular level so far. In the present study, the non-neuronal monoamine transporters, organic cation transporter (OCT) 1, OCT2, and extraneuronal monoamine transporter (EMT) (gene symbolsSLC22A1–A3), both from human and rat, were examined, stably expressed in 293 cells, for [3H]agmatine transport. Our results indicate that OCT2 and EMT, but not OCT1, efficiently translocate agmatine. The structural homolog putrescine was not accepted as substrate. Uptake of agmatine via EMT and OCT2 was saturable, with Kmvalues of 1 to 2 mM. The affinity of OCT1 was 10-fold lower. Carrier-mediated efflux of agmatine was documented in atrans-stimulation experiment. Finally, uptake of agmatine increased dramatically with increasing pH. Thus, only the singly charged species of agmatine is accepted as substrate. In conclusion, both EMT and OCT2 must be considered for the control of agmatine levels in rat and human.

Footnotes

  • Supported by Deutsche Forschungsgemeinschaft (SCHO 373/4-1 and SCH3-3).

  • DOI: 10.1124/jpet.102.044404

  • Abbreviations:
    EMT, extraneuronal monoamine transporter
    OCT
    organic cation transporter
    MPP+
    1-methyl-4-phenylpyridinium
    RT-PCR
    reverse transcriptase polymerase chain reaction
    h and r
    attached to a protein name, designate species as being human or rat, respectively
    • Received September 16, 2002.
    • Accepted October 30, 2002.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 304 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 304, Issue 2
1 Feb 2003
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Research ArticleCELLULAR AND MOLECULAR

Agmatine Is Efficiently Transported by Non-Neuronal Monoamine Transporters Extraneuronal Monoamine Transporter (EMT) and Organic Cation Transporter 2 (OCT2)

Dirk Gründemann, Christian Hahne, Reinhard Berkels and Edgar Schömig
Journal of Pharmacology and Experimental Therapeutics February 1, 2003, 304 (2) 810-817; DOI: https://doi.org/10.1124/jpet.102.044404

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Research ArticleCELLULAR AND MOLECULAR

Agmatine Is Efficiently Transported by Non-Neuronal Monoamine Transporters Extraneuronal Monoamine Transporter (EMT) and Organic Cation Transporter 2 (OCT2)

Dirk Gründemann, Christian Hahne, Reinhard Berkels and Edgar Schömig
Journal of Pharmacology and Experimental Therapeutics February 1, 2003, 304 (2) 810-817; DOI: https://doi.org/10.1124/jpet.102.044404
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