Novel histamine H3-receptor

Schlicker E, Kathmann M, Reidemeister S, Stark H, Schunack W (1994) Novel histamine H3 receptor antagonists affinities in an H3 receptor binding assay and potencies in two functional H3 receptor models. Br J Pharmacol 112 1043-1048 + 113 657 (erratum). 

Stark, H., Sadek, B., Krause, M., Huels, A., Ligneau, X., Ganellin, C. R., Arrang, J.-M., Schwartz, J.-C., Schunack, W. Novel Histamine H3-Receptor Antagonists with Carbonyl-Substituted 4-(3-(Phenoxy)propyl)-1H-imidazole Structures like Ciproxifan and Related Compounds. J. Med. Chem. 2000, 43, 3987-3994. 

A. Pharmacophore"based screening for novel histamine H3"receptor antagonists... 

Silver RB, Mackins CJ, Smith NCE, Koritchneva IL, Lefkowitz K, Lovenberg TW> Levi R Coupling of histamine H3 receptors to neuronal Na+/H+ exchange a novel protective mechanism in myocardial ischemia, Proc Natl Acad Sci USA 2001 98 2855. Silver RB, Poonwasi KS, Seyedi N, Wilson SJ, Lovenberg TW, Levi R Decreased intracellular calcium mediates the histamine H3-receptor-induced attenuation of norepinephrine exocytosis from cardiac sympathetic nerve endings. Proc Natl Acad Sci USA 2002 99 501. 

M. Krause, A. Rouleau, H. Stark, P. Luger, R. Lipp, M. Garbarg, J. C. Schwartz, W. Schunack, Synthesis, X-Ray Crystallography, and Pharmacokinetics of Novel Azome-thine Prodrugs of (R)-a-Methylhistamine Highly Potent and Selective Histamine H3 Receptor Agonists , J. Med. Chem. 1995, 38, 4070 - 4079. 

Howson W, Parsons ME, Raval P, Swayne GTG (1992) Two novel, potent and selective histamine H3 receptor agonists. Bioorg Med Chem Lett 2 77-78. 

Bertaccini, G., Coruzzi, G., Poli, E., 1991. Review article. The histamine H3 receptor A novel prejunctional receptor regulating gastrointestinal functions. Aliment. Pharmacol. Ther. 5,... 

Krause, M., Rouleau, A., Stark, H., Luger, P., Lipp, R., Garbarg, M. et al. 1995. Synthesis, X-ray cristallography, and pharmacokinetics of novel azomethine prodrugs of (R)a-methylhistamine highly potent and selective histamine H3 receptor agonists. J. Med. Chem. 38, 4070-4079. 

Imamura M, Lander HM, Levi R (1996b) Activation of histamine H3-receptors inhibits carrier-mediated norepinephrine release during protracted myocardial ischemia. Comparison with adenosine Ai-receptors and a2-adrenoceptors. Circ Res 78 475-81 Ishikawa S, Sperelakis N (1987) A novel class (H3) of histamine receptors on perivascular nerve terminals. Nature 327 158-60... 

Passani MB, Lin JS, Hancock A et al (2004) The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders. Trends Pharmacol Sci 25 618-625... 

Identification and optimization of a novel series of histamine H3 receptor antagonists... 

Design, synthesis, and evaluation of novel quinazolinone class of histamine H3 receptor inverse agonists... 

Histamine decarboxylase knockout mice are unable to produce histamine and these animals are unable to maintain wakefulness in a novel environment. Systemic or intraventricular administration of histamine or Hi receptor agonists induces wakefulness whereas systemic or intraventricular administration of Hi receptor antagonists induces sleep. Local administration of an H3 receptor agonist in the TMN induces sleep whereas local administration of an H3 receptor antagonist into the TMN induces wakefulness. 

Arrang, J. M., Garbarg, M. Schwartz, J. C. (1983). Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 302, 832-7. 

Drugs that act on the H3 receptor are being developed for the treatment of obesity, sleep disturbances, epilepsy and cognitive disorders. The ability of histamine to promote arousal, suppress appetite, elevate seizure threshold and stimulate cognitive processes implies that compounds able to enhance the release of neuronal histamine should mimic these effects. Several H3 antagonists currently in development demonstrate such activity and show promise as effective and novel therapeutic agents [40, 84-86]. Because H3 agonists suppress the release of... 

Ishikawa, S., Sperelakis, N., 1987. A novel class (H3) of histamine receptors on perivascular nerve terminals. Nature 327, 158-160. 

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