IMETIT DIHYDROBROMIDE

Description

Imetit is a histamine H₃ and H₄ receptor agonist (K_is = 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 (K_i = 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 .

The Uses of IMETIT DIHYDROBROMIDE

Imetit dihydrobromide is a high affinity agonist at the histamine H3- and H4-receptors.

What are the applications of Application

Imetit dihydrobromide is a high affinity agonist at the histamine H3- and H4-receptors

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™ .

Biochem/physiol Actions

Potent and selective H3 histamine receptor agonist.

Storage

Store at RT