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 Pharmacoljournal_title
European journal of pharmacologyauthors
Calcutt CR,Ganellin CR,Jackson B,Leigh BK,Owen DA,Smith IRdoi
10.1016/0014-2999(87)90206-8subject
Has Abstractpub_date
1987-01-06 00:00:00pages
65-74issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(87)90206-8journal_volume
133pub_type
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