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Literature summary for 2.6.1.7 extracted from

  • Linderholm, K.R.; Alm, M.T.; Larsson, M.K.; Olsson, S.K.; Goiny, M.; Hajos, M.; Erhardt, S.; Engberg, G.
    Inhibition of kynurenine aminotransferase II reduces activity of midbrain dopamine neurons (2016), Neuropharmacology, 102, 42-47.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one i.e. PF-04859989, selective inhibitor Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
neuron dopamine neuron Rattus norvegicus
-

General Information

General Information Comment Organism
physiological function acute administration of the KAT II inhibitor (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one is associated with a short-onset, time-dependent decrease in firing rate and burst activity of dopamine neurons, both parameters reaching a 50% reduction within 45 min. (3S)-3-Amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one reduces the number of spontaneously active dopamine cells. Pretreatment with D-cycloserine or [3-[[(3,4-dichlorophenyl)methyl]amino]propyl](diethoxy-methyl) phosphinic acid (CGP-52432) prevents the inhibitory action of (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one. Pretreatment with methyllycaconitine does not change the response, whereas picrotoxin partially prevents the inhibitory effects of (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one Rattus norvegicus