Evidence for low brain penetration by the H1-receptor antagonist temelastine (SK&F 93944)

Eur J Pharmacol. 1987 Jan 6;133(1):65-74. doi: 10.1016/0014-2999(87)90206-8.


Competition by the potent selective H1-receptor antagonist temelastine (SK & F 93944) with [3H]mepyramine binding to mouse cortex H1-receptors has been measured in vitro and vivo. The data were compared with that obtained using the classical H1-receptor antagonists mepyramine and promethazine and indicated that temelastine has relatively low ability to penetrate the blood-brain barrier compared with the latter two compounds. These studies also revealed that temelastine has relatively low affinity for mouse cortex H1-receptors compared with its affinity for H1-receptors in guinea-pig ileum and cortex, suggesting that it may be a useful compound with which to investigate potential H1-receptor tissue and species-related differences.

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism*
  • Dose-Response Relationship, Drug
  • Histamine H1 Antagonists / metabolism*
  • In Vitro Techniques
  • Male
  • Mice
  • Motor Activity / drug effects
  • Promethazine / pharmacology
  • Pyrilamine / metabolism
  • Pyrimidinones / metabolism*
  • Pyrimidinones / pharmacology
  • Receptors, Histamine H1 / metabolism
  • Tritium


  • Histamine H1 Antagonists
  • Pyrimidinones
  • Receptors, Histamine H1
  • Tritium
  • temelastine
  • Promethazine
  • Pyrilamine