Multiple mode of binding of phencyclidines: high affinity association between phencyclidine receptors in rat brain and a monovalent ion-sensitive polypeptide.
Two populations of phencyclidine (PCP) binding sites are shown to exist in the rat brain: a high-affinity monovalent ion-sensitive site (Kd of 10-14 nM for [3H]TCP, [3H]N-[1-(2-thienyl)cyclohexyl]piperidine), which exists in both the frontal cortex and the hippocampus, and a lower affinity site (Kd of 80-130 nM for [3H]TCP) which is found in the hippocampus but not in the frontal cortex. The nature of the interactions between the ion-binding sites and the high affinity PCP receptors depend on both ligand structure (PCP or TCP) and the ion involved (K' or Na'). The high-affinity sites are associated with an Mr 90,000 polypeptide whose labeling by [3H]azido phencyclidine is selectively inhibited by monovalent ions.
D000818:Animals; D001665:Binding Sites; D001923:Brain Chemistry; D005625:Frontal Lobe / Q000032:analysis; D006624:Hippocampus / Q000032:analysis; D066298:In Vitro Techniques; D007473:Ion Channels / Q000502:physiology; D008970:Molecular Weight; D010455:Peptides / Q000032:analysis*; D010622:Phencyclidine / Q000031:analogs & derivatives / Q000378:metabolism; D051381:Rats; D017981:Receptors, Neurotransmitter / Q000032:analysis*; D017478:Receptors, Phencyclidine; D012965:Sodium Chloride / Q000494:pharmacology; D014316:Tritium
D007473:Ion Channels; D010455:Peptides; D017981:Receptors, Neurotransmitter; D017478:Receptors, Phencyclidine; D014316:Tritium; D012965:Sodium Chloride; C012058:tenocyclidine; D010622:Phencyclidine