4-Acetoxy-7-chloro-3-(3-(-4-[11C]methoxybenzyl)phenyl)-2(1H)-quinolone

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Leung K

4-Acetoxy-7-chloro-3-(3-(-4-[11C]methoxybenzyl)phenyl)-2(1H)-quinolone

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PubMed ID
20641908 [ View in PubMed
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Abstract

N-Methyl D-aspartate (NMDA) receptor is an ionotropic receptor for glutamate playing an important role in synaptic plasticity, which is a cellular mechanism for learning and memory (1). The NMDA receptor forms a heterotetramer between two NR1 and two NR2 subunits with multiple regulatory binding sites for glutamate, glycine, Mg2+, polyamine, and drugs such as phencyclidine (PCP) (2). Overactivation of NMDA receptor has been suggested to be involved in a variety of neurological diseases such as ischemia, schizophrenia, Parkinson's disease, Huntington's disease, and epilepsy. 4-Hydroxy-7-chloro-3-(3-(-4-methoxybenzyl)phenyl)-2(1H)-quinolone (L703,717), a 4-hydroxyquinolone, is a potent antagonist for the glycine-binding site of the NMDA receptor, but it is poorly taken up by the brain because of its tight binding to serum albumin (3). Haradahira et al. (4) introduced an ester to the 4-hydroxyquinolone moiety to improve its penetration through the blood-brain barrier. 4-Acetoxy-7-chloro-3-(3-(-4-methoxybenzyl)phenyl)-2(1H)-quinolone (AcL703,717) taken up by the brain can be expected to be hydrolyzed to L703,717 by esterase in the brain. [11C]AcL703,717 is being evaluated as a positron emission tomography (PET) radioligand to study NMDA receptor in the brain.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
RolicyclidineGlutamate receptor ionotropic, NMDA 3AProteinHumans
Yes
Not AvailableDetails