Selective activation of Dopamine D3 receptors and norepinephrine transporter blockade enhances sustained attention.
Animals
Attention
/ physiology
Butylamines
/ antagonists & inhibitors
Cells, Cultured
Dopamine
/ metabolism
Dose-Response Relationship, Drug
Male
Motor Activity
/ drug effects
Norepinephrine
/ metabolism
Norepinephrine Plasma Membrane Transport Proteins
/ antagonists & inhibitors
Prazosin
/ pharmacology
Prefrontal Cortex
/ metabolism
Raclopride
/ pharmacology
Rats
Receptors, Dopamine D3
/ agonists
Catecholamine
Dopamine D3R agonist
Dopamine transporter
Executive function
Locomotor activity
Methylphenidate
Microdialysis
Norepinephrine transporter inhibitor
Sustained attention
Journal
Neuropharmacology
ISSN: 1873-7064
Titre abrégé: Neuropharmacology
Pays: England
ID NLM: 0236217
Informations de publication
Date de publication:
04 2019
04 2019
Historique:
received:
18
06
2018
revised:
28
12
2018
accepted:
06
01
2019
pubmed:
12
1
2019
medline:
28
12
2019
entrez:
12
1
2019
Statut:
ppublish
Résumé
Catecholamine transmitters dopamine (DA) and norepinephrine (NE) regulate prefrontal cortical (PFC) circuit activity and PFC-mediated executive functions. Accordingly, pharmacological agents that influence catecholamine neurotransmission exert prominent effects on cognition. Many such agents are used clinically to treat attention disorders. For example, methylphenidate blocks DA and NE reuptake and is the leading choice for attention deficit hyperactivity disorder (ADHD) treatment. Recently, we have designed SK609 - a selective small molecule agonist of the DA D3 receptor (D3R). In this study, we further characterized SK609's ability to selectively inhibit the reuptake of NE by NE transporters (NET). Our results indicate SK609 selectively inhibits NET with a K
Identifiants
pubmed: 30633928
pii: S0028-3908(19)30002-4
doi: 10.1016/j.neuropharm.2019.01.003
pmc: PMC6424628
mid: NIHMS1006809
pii:
doi:
Substances chimiques
4-(2-chlorophenyl)butan-2-amine
0
Butylamines
0
Norepinephrine Plasma Membrane Transport Proteins
0
Receptors, Dopamine D3
0
Raclopride
430K3SOZ7G
Dopamine
VTD58H1Z2X
Norepinephrine
X4W3ENH1CV
Prazosin
XM03YJ541D
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
178-188Subventions
Organisme : NIDA NIH HHS
ID : R01 DA017960
Pays : United States
Organisme : NIDA NIH HHS
ID : R01 DA019676
Pays : United States
Organisme : NIDA NIH HHS
ID : R01 DA031900
Pays : United States
Organisme : NIMH NIH HHS
ID : R01 MH106912
Pays : United States
Informations de copyright
Copyright © 2019 Elsevier Ltd. All rights reserved.
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