In vivo labelling of the NMDA receptor channel complex by [3H]MK-801.
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.
Price
G W
GW
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, U.K.
Ahier
R G
RG
Middlemiss
D N
DN
Singh
L
L
Tricklebank
M D
MD
Wong
E H
EH
D000345:Affinity Labels; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001224:Aspartic Acid / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors; D001665:Binding Sites / Q000187:drug effects; D001667:Binding, Competitive; D003986:Dibenzocycloheptenes / Q000494:pharmacology*; D004148:Dioxolanes / Q000494:pharmacology; D016291:Dizocilpine Maleate; D007473:Ion Channels / Q000378:metabolism* / Q000502:physiology; D008297:Male; D051379:Mice; D016202:N-Methylaspartate; D010620:Phenazocine / Q000031:analogs & derivatives / Q000494:pharmacology; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter / Q000378:metabolism* / Q000502:physiology; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control
D000345:Affinity Labels; D000927:Anticonvulsants; D003986:Dibenzocycloheptenes; D004148:Dioxolanes; D007473:Ion Channels; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; D001224:Aspartic Acid; D016202:N-Methylaspartate; D016291:Dizocilpine Maleate; C012134:SK&F 10047; D010620:Phenazocine