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Neurotransmitter Transporters pp 151–180Cite as

Extraneuronal Monoamine Transporter and Organic Cation Transporters 1 and 2: A Review of Transport Efficiency

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Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 175))

Abstract

The extraneuronal monoamine transporter (EMT) corresponds to the classical steroid-sensitivemonoamine transportmechanism that was first described as “uptake2” in rat heart with noradrenaline as substrate. The organic cation transporters OCT1 and OCT2 are related to EMT. The three carriers share basic structural and functional characteristics. Hence, EMT, OCT1 and OCT2 constitute a group referred to as non-neuronal monoamine transporters or organic cation transporters. After a brief general introduction, this review focuses on the critical analysis of substrate specificity. We calculate from the available literature and compare consensus transport efficiency (clearance) data for human and rat EMT, OCT1 and OCT2, expressed in transfected cell lines. From the plethora of inhibitors that have been tested, the casual observer likely gets the impression that these carriers indiscriminately transport very many compounds. However, our knowledge about actual substrates is rather limited. 1-Methyl-4-phenylpyridinium (MPP+) is an excellent substrate for all three carriers, with clearances typically in the range of 20-50 μl min−1 mg protein−1. The secondbest general substrate is tyramine with a transport efficiency (TE) range relative to MPP+ of 20%–70%. The TEs of OCT1 and OCT2 for dopamine, noradrenaline, adrenaline and 5-HT in general are rather low, in the range relative to MPP+ of 5%–15%. This suggests that OCT1 and OCT2 are not primarily dedicated to transport these monoamine transmitters; only EMT may play a significant role in catecholamine inactivation. Formany substrates, such as tetraethylammonium, histamine, agmatine, guanidine, cimetidine, creatinine, choline and acetylcholine, the transport efficiencies are markedly different among the carriers.

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    PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    Google Scholar 

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    PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    Article  PubMed  CAS  Google Scholar 

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    PubMed  Google Scholar 

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    Article  PubMed  Google Scholar 

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Authors and Affiliations

  1. Department of Pharmacology, University of Cologne, Gleueler Straße 24, 50931, Cologne, Germany

    E. Schömig, A. Lazar & D. Gründemann

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  1. E. Schömig
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  2. A. Lazar
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  3. D. Gründemann
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  1. Institute of Pharmacology Center for Biomolecular Medicine and Pharmacology, Medical University Vienna, Waehringer Str. 13a, A-1090, Wien, Austria

    Harald H. Sitte  & Michael Freissmuth  & 

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Schömig, E., Lazar, A., Gründemann, D. (2006). Extraneuronal Monoamine Transporter and Organic Cation Transporters 1 and 2: A Review of Transport Efficiency. In: Sitte, H.H., Freissmuth, M. (eds) Neurotransmitter Transporters. Handbook of Experimental Pharmacology, vol 175. Springer, Berlin, Heidelberg. https://doi.org/10.1007/3-540-29784-7_8

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