Phencyclidine blocks histamine H3-receptors in rat brain

Eur J Pharmacol. 1988 Nov 15;157(1):31-5. doi: 10.1016/0014-2999(88)90467-0.


Phencyclidine (PCP) was examined for its ability to modulate histamine release from rat brain slices labeled with L-[3H]histidine. PCP failed to mimic but completely reversed the autoinhibitory effect of histamine at H3-receptors with an apparent Ki value of 13 +/- 3 microM. A direct interaction of PCP with H3-autoreceptors rather than PCP or sigma receptor sites was confirmed by binding studies. PCP inhibited the binding of [3H](R)alpha-methylhistamine to H3-receptor sites in rat cerebral membranes with a Ki value of 25 +/- 2 microM. It is concluded that PCP is a H3-receptor antagonist of moderate potency.

MeSH terms

  • Animals
  • Brain / drug effects*
  • Brain / metabolism
  • Histamine / metabolism*
  • In Vitro Techniques
  • Phencyclidine / pharmacology*
  • Rats
  • Receptors, Histamine / drug effects*
  • Receptors, Histamine H3


  • Receptors, Histamine
  • Receptors, Histamine H3
  • Histamine
  • Phencyclidine