RGD Reference Report - Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. - Rat Genome Database

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Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain.

Authors: Amphoux, Anne  Vialou, Vincent  Drescher, Eva  Brüss, Michael  Mannoury La Cour, Clotilde  Rochat, Catherine  Millan, Mark J  Giros, Bruno  Bönisch, Heinz  Gautron, Sophie 
Citation: Amphoux A, etal., Neuropharmacology. 2006 Jun;50(8):941-52. doi: 10.1016/j.neuropharm.2006.01.005. Epub 2006 Mar 31.
RGD ID: 155663558
Pubmed: PMID:16581093   (View Abstract at PubMed)
DOI: DOI:10.1016/j.neuropharm.2006.01.005   (Journal Full-text)

Organic cation transporters (OCTs) are polyspecific carriers implicated in low-affinity, corticosteroid-sensitive extraneuronal catecholamine uptake in peripheral tissues. The three main OCT subtypes, OCT1, OCT2 and OCT3, are also present in the brain, but their central role remains unclear. In the present study, we investigated by comparative in situ hybridization analysis the regional distribution of these transporters in rat brain and compared their functional properties in stably transfected HEK293 cells expressing human or rat OCTs. In rat brain, OCT2 and OCT3 mRNAs are expressed predominantly in regions located at the brain-cerebrospinal fluid border, with OCT3 mRNA expression extending to regions that belong to monoaminergic pathways such as raphe nuclei, striatum and thalamus. After normalization with MPP+ uptake, OCT2 and OCT3 subtypes share a similar monoamine preference profile, with higher transport efficacies for epinephrine and histamine than for the other monoamines. Interestingly, a significant level of epinephrine transport, previously only shown for rOCT2, is achieved by most OCTs subtypes. Finally, another novel finding was that OCTs are sensitive to 3,4-methylenedioxymetamphetamine (MDMA), phencyclidine (PCP), MK-801 and ketamine. Altogether, all our results suggest a functional specialization of OCT subtypes, based both on their intrinsic properties and their differential regional expression pattern in the brain.

Gene Ontology Annotations    Click to see Annotation Detail View

Biological Process

Molecular Function

Objects Annotated

Genes (Rattus norvegicus)
Slc22a1  (solute carrier family 22 member 1)
Slc22a2  (solute carrier family 22 member 2)
Slc22a3  (solute carrier family 22 member 3)


Additional Information