Imetit is a histamine H3 and H4 receptor agonist (Kis = 0.3 and 2.7 nM, respectively, in radioligand binding assays). It is selective for histamine H3 and H4 receptors over H1 and H2 receptors at concentrations up to 100 μM, as well as the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 240 nM)., Imetit reduces potassium-induced increases in histamine levels in isolated rat cerebral cortex slices (EC50 = 2.8 nM). It increases scratching in mice (ED50 = 0.9 μmol), an effect that is reduced by the H3 receptor antagonist thioperamide .
Imetit dihydrobromide is a high affinity agonist at the histamine H3- and H4-receptors.
ChEBI: A hydrobromide salt obtained by reaction of imetit with two equivalents of hydrobromic acid. An extremely potent, high affinity agonist at H3 and H4 receptors (Ki values are 0.3 and 2.7 nM respectively). Induces sh
pe change in eosinophils with an EC50 of 25 nM. Centrally active following systemic administration.
An extremely potent, high affinity agonist at H 3 and H 4 receptors (K i values are 0.3 and 2.7 nM respectively). Induces shape change in eosinophils with an EC 50 of 25 nM. Centrally active following systemic administration. Also available as part of the Histamine H 3 Receptor Tocriset™ .
Potent and selective H3 histamine receptor agonist.
