The histamine H3 receptor: a general presynaptic histaminergic regulatory system?

H3 receptor antagonist, thioperamide, inhibits adrenal steroidogenesis and histamine binding to adrenocortical microsomes and binds to cytochrome P450

“…H1c exhibits strong preference for certain novel, antioestrogen-like compounds, lesser affinity for HI ligands and very low affinity for H2 ligands (Brandes et al, 1990). An important locus for H3 receptors is presynaptic nerve terminals; histamine and other H3 agonists reportedly interact at these receptors to suppress the synthesis and release of histamine (van Der Werf et al, 1989). We show here that the H3 antagonist, thioperamide (Arrang et al, 1987b), is a potent competitor of histamine binding to low affinity microsomal Hjc; in adrenal microsomes at least some proportion of the microsomal binding sites represents P450 enzymes; and inhibition of adrenal steroidogenesis is a prominent pharmacological response to thioperamide.…”

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

“…H 3 receptormediated inhibition of histamine release has also been observed in human cerebral cortex (Arrang et al, 1988b). Differences in the distribution of H 3 receptor binding sites and the levels of histidine decarboxylase (an index of histaminergic nerve terminals) suggested at an early stage that H 3 receptors were not confined to histamine-containing neurons within the mammalian CNS (Arrang et al, 1987a;van der Werf and Timmerman, 1989). This has been confirmed by the observations that H 3 receptors can regulate serotonergic (Schlicker et al, 1988(Schlicker et al, , 1989Threlfell et al, 2004), noradrenergic (Schlicker et al, 1989), cholinergic (Clapham and Kilpatrick, 1992), and dopaminergic (Schlicker et al, , 1993Munari et al, 2013) neurotransmitter release in mammalian brain.…”

R‐α‐methylhistamine‐induced inhibition of gastric acid secretion in pylorus‐ligated rats via central histamine H3 receptors

“…Subsequently, pharmacological studies, performed both on central and peripheral tissues with the highly selective H3 agonist, R-a-methylhistamine, and antagonist, thioperamide, have shown that the third histamine receptor is also localized in non-histaminergic neurones (van der Werf & Timmerman, 1989) and in extraneuronal sites (Ea Kim et al, 1992;Schworer et al, 1992;Cardell & Edvinsson, 1994).…”