The binding of [3H]thienyl cyclohexylpiperidine ([3H]TCP) to the NMDA-phencyclidine receptor complex.
The high affinity binding of the phencyclidine derivative [3H]TCP to cortical membranes of the rat was investigated. In an extensively washed membrane preparation the binding of [3H]TCP was enhanced in the presence of L-glutamate and NMDA. The stimulation of the binding of [3H]TCP by L-glutamate was inhibited competitively by AP5 and non-competitively by MK801. The binding of [3H]TCP was also enhanced in the presence of glycine; this effect was insensitive to strychnine and inhibited non-competitively by AP5. Saturation experiments demonstrated that MK801 was a competitive inhibitor of the binding of [3H]TCP. These results suggest that [3H]TCP binds to a site similar to that which binds MK801; this site may be associated with the ion channel of the NMDA receptor.
Stirling
J M
JM
Astra Neuroscience Research Unit, London, U.K.
Cross
A J
AJ
Green
A R
AR
D000596:Amino Acids / Q000494:pharmacology; D000818:Animals; D005971:Glutamates / Q000494:pharmacology; D005998:Glycine / Q000494:pharmacology; D013287:Illicit Drugs / Q000378:metabolism*; D008297:Male; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism*; D011957:Receptors, Opioid / Q000378:metabolism*; D017478:Receptors, Phencyclidine
D000596:Amino Acids; D005971:Glutamates; D013287:Illicit Drugs; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; D011957:Receptors, Opioid; D017478:Receptors, Phencyclidine; C012058:tenocyclidine; D010622:Phencyclidine; D005998:Glycine