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  • Title: In vivo labelling of the NMDA receptor channel complex by [3H]MK-801.
    Author: Price GW, Ahier RG, Middlemiss DN, Singh L, Tricklebank MD, Wong EH.
    Journal: Eur J Pharmacol; 1988 Dec 13; 158(3):279-82. PubMed ID: 2472964.
    Abstract:
    An in vivo radioligand binding assay for the N-methyl-D-aspartate (NMDA) receptor channel complex in the mouse brain has been developed using the non-competitive NMDA receptor antagonist [3H]MK-801. In vivo binding of [3H]MK-801 was displaced by MK-801 (ED50 = 0.17 mg/kg i.p.), (-)-MK-801 (1.0 mg/kg), thienylcyclohexylpiperidine (1.8 mg/kg), etoxadrol (5.1 mg/kg) and (+)-SKF 10,047 (34.5 mg/kg). The potency of these drugs in this in vivo binding assay was highly correlated (r = 0.97) with their functional effects as antagonists of N-methyl-DL-aspartate-induced tonic convulsions.
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