Effects of isofloxythepin on central and peripheral histamine systems

K. Saeki, R. Oishi, Masahiro Nishibori, Y. Itoh

Research output: Contribution to journalArticle

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Abstract

The effects of isofloxythepin, a dibenzo[b,f]thiepin derivative, on the central and peripheral histamine systems were compared with those of chlorpromazine and haloperidol. The three drugs examined all inhibited both the histamine-induced contraction of guinea pig ileum and the specific [3H]mepyramine binding to guinea pig brain membranes in a dose-dependent manner. The effectiveness in inhibiting these reactions was in the order of: chlorpromazine > isofloxythepin > haloperidol. The histamine-induced relaxation of rat uterus, which is mediated by H2-receptors, was not affected by isofloxythepin. The effect of isofloxythepin on the pargyline-induced accumulation of tele-methylhistamine in the mouse brain was indicative of a decrease in histamine turnover, whereas chlorpromazine and haloperidol were devoid of such effects. Isofloxythepin inhibited both the lethal effect of histamine injected i.v. in mice and histamine-induced edema in rat hind paws for more strongly than chlorpromazine or haloperidol did. These results show that isofloxythepin is a neuroleptic with H1-antagonist properties, which are intermediate in potency between those of chlorpromazine and haloperidol, and also it may have an inhibitory action on histamine turnover in the brain. Protection against the lethal effect of histamine and the inhibition of histamine edema by isofloxythepin may largely be due to mechanisms other than the blocking of H1-receptors.

Original languageEnglish
Pages (from-to)55-62
Number of pages8
JournalJapanese Journal of Pharmacology
Volume50
Issue number1
Publication statusPublished - 1989

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Histamine
Chlorpromazine
Haloperidol
Thiepins
Edema
Brain
Guinea Pigs
Pargyline
Pyrilamine
isofloxythepin
Histamine H1 Receptors
Histamine H2 Receptors
Ileum
Antipsychotic Agents
Uterus
Membranes
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Pharmacology

Cite this

Effects of isofloxythepin on central and peripheral histamine systems. / Saeki, K.; Oishi, R.; Nishibori, Masahiro; Itoh, Y.

In: Japanese Journal of Pharmacology, Vol. 50, No. 1, 1989, p. 55-62.

Research output: Contribution to journalArticle

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abstract = "The effects of isofloxythepin, a dibenzo[b,f]thiepin derivative, on the central and peripheral histamine systems were compared with those of chlorpromazine and haloperidol. The three drugs examined all inhibited both the histamine-induced contraction of guinea pig ileum and the specific [3H]mepyramine binding to guinea pig brain membranes in a dose-dependent manner. The effectiveness in inhibiting these reactions was in the order of: chlorpromazine > isofloxythepin > haloperidol. The histamine-induced relaxation of rat uterus, which is mediated by H2-receptors, was not affected by isofloxythepin. The effect of isofloxythepin on the pargyline-induced accumulation of tele-methylhistamine in the mouse brain was indicative of a decrease in histamine turnover, whereas chlorpromazine and haloperidol were devoid of such effects. Isofloxythepin inhibited both the lethal effect of histamine injected i.v. in mice and histamine-induced edema in rat hind paws for more strongly than chlorpromazine or haloperidol did. These results show that isofloxythepin is a neuroleptic with H1-antagonist properties, which are intermediate in potency between those of chlorpromazine and haloperidol, and also it may have an inhibitory action on histamine turnover in the brain. Protection against the lethal effect of histamine and the inhibition of histamine edema by isofloxythepin may largely be due to mechanisms other than the blocking of H1-receptors.",
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