[3H]PCP-3-OH and (+)[3H]SKF 10047 binding sites in rat brain membranes: evidence of multiplicity

Eur J Pharmacol. 1987 Apr 14;136(2):231-4. doi: 10.1016/0014-2999(87)90715-1.

Abstract

Specific binding of one of the most potent analogs of phencyclidine (PCP), [3H]PCP-3-OH, in rat brain membranes revealed the labeling of high (Kd = 0.5 nM) and low (Kd = 16 nM) affinity binding sites. (+)SKF 10047 potently inhibited high, but not low, affinity [3H]PCP-3-OH binding. (+)[3H]SKF 10047 apparently labeled the high affinity PCP-3-OH binding site and also an additional site, sensitive to haloperidol, which is distinct from the two sites labeled by [3H]PCP-3-OH.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Binding, Competitive / drug effects
  • Brain / metabolism*
  • Haloperidol / pharmacology
  • In Vitro Techniques
  • Phenazocine / analogs & derivatives*
  • Phenazocine / metabolism
  • Phencyclidine / analogs & derivatives*
  • Phencyclidine / metabolism
  • Rats
  • Receptors, Neurotransmitter / metabolism*
  • Receptors, Phencyclidine

Substances

  • Receptors, Neurotransmitter
  • Receptors, Phencyclidine
  • SK&F 10047
  • 3-hydroxyphencyclidine
  • Phenazocine
  • Phencyclidine
  • Haloperidol