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

Abstract:

: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.

journal_name

Eur J Pharmacol

authors

Calcutt CR,Ganellin CR,Jackson B,Leigh BK,Owen DA,Smith IR

doi

10.1016/0014-2999(87)90206-8

subject

Has Abstract

pub_date

1987-01-06 00:00:00

pages

65-74

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(87)90206-8

journal_volume

133

pub_type

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