Description
Imetit is a histamine H
3 and H
4 receptor agonist (K
is = 0.3 and 2.7 nM, respectively, in radioligand binding assays). It is selective for histamine H
3 and H
4 receptors over H
1 and H
2 receptors at concentrations up to 100 μM, as well as the serotonin (5-HT) receptor subtype 5-HT
3 (K
i = 240 nM)., Imetit reduces potassium-induced increases in histamine levels in isolated rat cerebral cortex slices (EC
50 = 2.8 nM). It increases scratching in mice (ED
50 = 0.9 μmol), an effect that is reduced by the H
3 receptor antagonist thioperamide .
Definition
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.
Biological Activity
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™ .
