Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
, 503 (1), 68-72

Evaluation of Brain Pharmacokinetics of (+)MK-801 in Relation to Behaviour

Affiliations

Evaluation of Brain Pharmacokinetics of (+)MK-801 in Relation to Behaviour

Nico Wegener et al. Neurosci Lett.

Abstract

The non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist (+)MK-801 is widely used in animal research (over 3000 publications), however its extracellular brain concentration has never been reported. Here, we show using in vivo microdialysis that systemic injection of (+)MK-801 at doses of 0.05, 0.1 or 0.2mg/kg resulted in peak brain ECF concentration of 6, 14 or 34 nM, respectively. Moreover, (+)MK-801 resulted in a dose-dependent learning impairment in the Morris water maze as well as hyperactivity in the open field. These data demonstrate for the first time that (+)MK-801 at doses producing behavioural alterations expected from NMDA receptor blockade reaches extracellular brain concentrations corresponding to the affinity at NMDA receptors.

Similar articles

See all similar articles

Cited by 11 PubMed Central articles

See all "Cited by" articles

MeSH terms

Substances

LinkOut - more resources

Feedback