PMID- 16581093
OWN - NLM
STAT- MEDLINE
DCOM- 20060928
LR  - 20131121
IS  - 0028-3908 (Print)
IS  - 0028-3908 (Linking)
VI  - 50
IP  - 8
DP  - 2006 Jun
TI  - Differential pharmacological in vitro properties of organic cation transporters 
      and regional distribution in rat brain.
PG  - 941-52
AB  - 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.
FAU - Amphoux, Anne
AU  - Amphoux A
AD  - Institut National de la Sante et de la Recherche Medicale U513, Faculte de 
      Medecine, Universite Paris XII, D-94010 Creteil, France.
FAU - Vialou, Vincent
AU  - Vialou V
FAU - Drescher, Eva
AU  - Drescher E
FAU - Bruss, Michael
AU  - Bruss M
FAU - Mannoury La Cour, Clotilde
AU  - Mannoury La Cour C
FAU - Rochat, Catherine
AU  - Rochat C
FAU - Millan, Mark J
AU  - Millan MJ
FAU - Giros, Bruno
AU  - Giros B
FAU - Bonisch, Heinz
AU  - Bonisch H
FAU - Gautron, Sophie
AU  - Gautron S
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20060331
PL  - England
TA  - Neuropharmacology
JT  - Neuropharmacology
JID - 0236217
RN  - 0 (Biogenic Monoamines)
RN  - 0 (Dopamine Uptake Inhibitors)
RN  - 0 (Excitatory Amino Acid Agonists)
RN  - 0 (Excitatory Amino Acid Antagonists)
RN  - 0 (Organic Cation Transport Proteins)
RN  - 0 (RNA, Messenger)
RN  - 10028-17-8 (Tritium)
RN  - 6384-92-5 (N-Methylaspartate)
RN  - CK833KGX7E (Amphetamine)
RN  - I5Y540LHVR (Cocaine)
SB  - IM
MH  - Amphetamine/pharmacology
MH  - Animals
MH  - Biogenic Monoamines/pharmacokinetics
MH  - Brain/drug effects/*metabolism
MH  - Cell Line
MH  - Cocaine/pharmacology
MH  - Dopamine Uptake Inhibitors/pharmacology
MH  - Dose-Response Relationship, Drug
MH  - Drug Interactions
MH  - Excitatory Amino Acid Agonists/pharmacology
MH  - Excitatory Amino Acid Antagonists/pharmacology
MH  - Female
MH  - Humans
MH  - In Situ Hybridization/methods
MH  - N-Methylaspartate/pharmacology
MH  - Organic Cation Transport Proteins/classification/genetics/*metabolism
MH  - Protein Binding/drug effects
MH  - RNA, Messenger/metabolism
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Transfection/methods
MH  - Tritium/pharmacokinetics
EDAT- 2006/04/04 09:00
MHDA- 2006/09/29 09:00
CRDT- 2006/04/04 09:00
PHST- 2005/10/31 00:00 [received]
PHST- 2006/01/17 00:00 [revised]
PHST- 2006/01/19 00:00 [accepted]
PHST- 2006/04/04 09:00 [pubmed]
PHST- 2006/09/29 09:00 [medline]
PHST- 2006/04/04 09:00 [entrez]
AID - S0028-3908(06)00019-0 [pii]
AID - 10.1016/j.neuropharm.2006.01.005 [doi]
PST - ppublish
SO  - Neuropharmacology. 2006 Jun;50(8):941-52. doi: 10.1016/j.neuropharm.2006.01.005. 
      Epub 2006 Mar 31.