Comparative analysis of novel decynium-22 analogs to inhibit transport by the low-affinity, high-capacity monoamine transporters, organic cation transporters 2 and 3, and plasma membrane monoamine transporter.
Antidepressants
Decynium-22
Monoamine uptake
Organic cation transporters
Plasma membrane monoamine transporter
Transporter inhibition
Journal
European journal of pharmacology
ISSN: 1879-0712
Titre abrégé: Eur J Pharmacol
Pays: Netherlands
ID NLM: 1254354
Informations de publication
Date de publication:
05 Jan 2019
05 Jan 2019
Historique:
received:
09
08
2018
revised:
03
10
2018
accepted:
19
10
2018
pubmed:
27
11
2018
medline:
5
2
2019
entrez:
27
11
2018
Statut:
ppublish
Résumé
Growing evidence supports involvement of low-affinity/high-capacity organic cation transporters (OCTs) and plasma membrane monoamine transporter (PMAT) in regulating clearance of monoamines. Currently decynium-22 (D22) is the best pharmacological tool to study these transporters, however it does not readily discriminate among them, underscoring a need to develop compounds with greater selectivity for each of these transporters. We developed seven D22 analogs, and previously reported that some have lower affinity for α1-adrenoceptors than D22 and showed antidepressant-like activity in mice. Here, we extend these findings to determine the affinity of these analogs for OCT2, OCT3 and PMAT, as well as serotonin, norepinephrine and dopamine transporters (SERT, NET and DAT) using a combination of uptake competition with [
Identifiants
pubmed: 30473490
pii: S0014-2999(18)30613-7
doi: 10.1016/j.ejphar.2018.10.028
pmc: PMC6440482
mid: NIHMS1513191
pii:
doi:
Substances chimiques
Equilibrative Nucleoside Transport Proteins
0
Octamer Transcription Factor-3
0
Organic Cation Transporter 2
0
POU5F1 protein, human
0
Quinolines
0
SLC29A4 protein, human
0
pseudoisocyanine
20766-49-8
Types de publication
Comparative Study
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
351-364Subventions
Organisme : NIGMS NIH HHS
ID : K12 GM111726
Pays : United States
Organisme : NIMH NIH HHS
ID : R01 MH093320
Pays : United States
Organisme : NIDA NIH HHS
ID : T32 DA031115
Pays : United States
Organisme : Austrian Science Fund FWF
ID : W 1232
Pays : Austria
Informations de copyright
Copyright © 2018 Elsevier B.V. All rights reserved.
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