4-(1H-IMIDAZOL-4-YLMETHYL)PIPERIDINE DIHYDROBROMIDE

Description

Immepip is a histamine H₃ receptor agonist (K_I = 0.4 nM in SK-N-MC cell membranes expressing the human receptor). It is selective for histamine H₃ over H₁ and H₂ receptors in CHO cell membranes expressing the guinea pig and human receptors, respectively (K_is = >16 μM for both) but also agonizes H₄ receptors (K_I = 9 nM in SK-N-MC cell membranes expressing the human receptor). Immepip (5 mg/kg, s.c.) decreases hypothalamic histamine release in anesthetized rats. It decreases flinching in the formalin test in rats when administered at doses of 5 and 30 mg/kg and inhibits formalin-induced paw edema at 30 mg/kg.

Chemical Properties

Crystalline Solid

Uses

A selective nonchiral histamine H3 agonist.

Biological Activity

Potent histamine H 3 receptor agonist. Also binds to H 4 receptors (K i values are 0.4 and 9 nM at human recombinant H 3 and H 4 receptors respectively). Equipotent to or slightly more active than (R)- α -methylhistamine at H 3 receptors.

storage

Desiccate at RT