MK-801 is an indirect antagonist of the NMDA excitatory amino acid receptor which is being considered for possible clinical development for treatment of epilepsy and stroke. MK-801 was evaluated for its effects on regional brain energy metabolism by means of Sokoloff's 2-deoxyglucose (2-DG) autoradiography method. MK-801 produced dramatic alterations in regional energy metabolism, exciting Papez circuit and dopaminergic structures most intensely. The pattern of metabolic alterations was virtually indistinguishable from that previously described for the psychotomimetic drug of abuse, phencyclidine (PCP). It is concluded that MK-801 is at risk for possibly producing PCP-like psychotomimetic effects.
This is a preview of subscription content, log in to check access.
Buy single article
Instant access to the full article PDF.
Price includes VAT for USA
Subscribe to journal
Immediate online access to all issues from 2019. Subscription will auto renew annually.
This is the net price. Taxes to be calculated in checkout.
Clineschmidt BV, Martin GE, Bunting PR (1982) Anticonvulsant activity of (+)-S-methyl-10,11-dihydro-5H-dibenzo (a, d) cyclohepten-5,10-imine (MK-801), a substance with potent anticonvulsant, central sympathomimetic, and apparent anxiolytic properties. Drug Dev Res 2:123
Iversen LL, Woodruff GN, Kemp JA, Foster AC, Gill R, Wong EHF (1988) Pharmacology and neuroprotective effects of the NMDA antagonist MK-801. In: Domino EF, Kamenka J-M (eds) Sigma and phencylidine-like compounds as molekular probes in biology. NPP Books, Ann Arbor, MI, p 757
Kemp JA, Priestley T, Woodruff GN (1986) MK-801, a novel orally-active anticonvulsant, is a potent non-competitive N-methyl-d-aspartate receptor antagonist. Br J Pharmacol [Proc Suppl] 89:535P
Lodge D, Aran JA, Church J, Davies SN, Martin D, O'Shaughnessy CT, Zemen S (1987) Excitatory amino acids and phencyclidine-like drugs. In: Hicks TP, Lodge D, McLennan H (eds) Excitatory amino acid transmission. Liss, New York, p 83
Piercey MF, RAy CA (1988) Dramatic limbic and cortical effects mediated by high affinity PCP receptors. Life Sci 43:379–385
About this article
Cite this article
Piercey, M.F., Hoffmann, W.E. & Kaczkofsky, P. Functional evidence for PCP-like effects of the anti-stroke candidate MK-801. Psychopharmacology 96, 561–562 (1988). https://doi.org/10.1007/BF02180042