The binding of [3H]thienyl cyclohexylpiperidine ([3H]TCP) to the NMDA-phencyclidine receptor complex

Neuropharmacology. 1989 Jan;28(1):1-7. doi: 10.1016/0028-3908(89)90059-2.

Abstract

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.

MeSH terms

  • Amino Acids / pharmacology
  • Animals
  • Glutamates / pharmacology
  • Glycine / pharmacology
  • Illicit Drugs / metabolism*
  • Male
  • Phencyclidine / analogs & derivatives*
  • Phencyclidine / metabolism
  • Rats
  • Rats, Inbred Strains
  • Receptors, N-Methyl-D-Aspartate
  • Receptors, Neurotransmitter / drug effects
  • Receptors, Neurotransmitter / metabolism*
  • Receptors, Opioid / metabolism*
  • Receptors, Phencyclidine

Substances

  • Amino Acids
  • Glutamates
  • Illicit Drugs
  • Receptors, N-Methyl-D-Aspartate
  • Receptors, Neurotransmitter
  • Receptors, Opioid
  • Receptors, Phencyclidine
  • tenocyclidine
  • Phencyclidine
  • Glycine