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Immepip is a histamine H3 receptor agonist (KI = 0.4 nM in SK-N-MC cell membranes expressing the human receptor).1 It is selective for histamine H3 over H1 and H2 receptors in CHO cell membranes expressing the guinea pig and human receptors, respectively (Kis = >16 μM for both) but also agonizes H4 receptors (KI = 9 nM in SK-N-MC cell membranes expressing the human receptor).2,1 Immepip (5 mg/kg, s.c.) decreases hypothalamic histamine release in anesthetized rats.3 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.4
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1. Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59(3), 420-426 (2001).
2. A new potent and selective histamine H3 receptor agonist, 4-
3. In vivo modulation of rat hypothalamic histamine release by the histamine H3 receptor ligands, immepip and clobenpropit. Effects of intrahypothalamic and peripheral application. Eur. J. Pharmacol. 362(2-3), 149-155 (1998).
4. Activation of peripheral and spinal histamine H3 receptors inhibits formalin-