Description
Immepip is a histamine H
3 receptor agonist (K
I = 0.4 nM in SK-N-MC cell membranes expressing the human receptor). It is selective for histamine H
3 over H
1 and H
2 receptors in CHO cell membranes expressing the guinea pig and human receptors, respectively (K
is = >16 μM for both) but also agonizes H
4 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.
References
[1] CHANGLU LIU. Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.[J]. Molecular Pharmacology, 2001, 59 3 1: 420-426. DOI:
10.1124/mol.59.3.420[2] ROELAND C. VOLLINGA. A New Potent and Selective Histamine H3 Receptor Agonist, 4-(1H-imidazol-4-ylmethyl)piperidine[J]. Journal of Medicinal Chemistry, 1994, 37 3: 332-333. DOI:
10.1021/jm00029a002[3] FRANK P JANSEN . In vivo modulation of rat hypothalamic histamine release by the histamine H3 receptor ligands, immepip and clobenpropit. Effects of intrahypothalamic and peripheral application[J]. European journal of pharmacology, 1998, 362 2: Pages 149-155. DOI:
10.1016/s0014-2999(98)00739-0[4] KERI E. CANNON Lindsay B H Rob Leurs. Activation of peripheral and spinal histamine H3 receptors inhibits formalin-induced inflammation and nociception, respectively[J]. Pharmacology Biochemistry and Behavior, 2007, 88 1: Pages 122-129. DOI:
10.1016/j.pbb.2007.07.014
