Human histamine H3 receptor

Lovenberg TW, Roland BL, Wilson SJ, Jiang X, Pyati 61 J, Huvar A, Jackson MR> Erlander MG Cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol 1999 55 1101. 

H, Boutin JA, Galizzi JP (2001) Genomic organization and characterization of splice variants of the human histamine H3 receptor. Biochem J 355 279-88... 

Ligneau, X. etal. BF2.649 [l- 3-[3-(4-Chlorophenyl)propoxy]propyl piperidine, hydrochloride], a nonimidazole inverse agonist/antago-nist at the human histamine H3 receptor preclinical pharmacology. J. Pharmacol. Exp. Therapeut. 2007, 320, 365-375. 

Ligneau, X., Morisset, S., Tardivel-Lacombe, T., Ghabou, F., Ganellin, C.R., et at. (2000) Distinct pharmacology of rat and human histamine H3 receptors role of two amino acids in the third transmembrane domain. Br. J. Pharmacol. 131 1247-1250. 

Imamura M, Seyedi N, Lander HM, Levi R Functional identification of histamine H3-receptors in the human heart. Circ Res 1995 77 206. 

Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R. Evaluation of histamine HI-, H2-, and H3-receptor ligands at the human histamine H4 receptor identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 2005 314 1310-21. 

As far as man is concerned, a presynaptic inhibition of the noradrenaline release by H3 receptors was only studied in the isolated human saphenous vein In this tissue, these receptors, similarly to a2-adrenoceptors, decrease the 3H-noradrenaline overflow elicited by electrical field stimulation (Molderings et al., 1992). Therefore, the role of histamine H3-receptors in the global control of the blood pressure in humans cannot be stated at present. 

Similarly to what identified in the rat, histamine H3 receptor activation does not contribute to prostacyclin production in coltured human endothelial cells (Bull et al., 1992). There are no findings explaining any possible involvement of these receptors in the control of endothelial functions in humans. 

Cherifi, Y., Pigeon, C., Le Romancer, M., Bado, A., Reyl-Desmars, F., Lewin, M.J.M., 1992. Purification of a histamine H3 receptor negatively coupled to phosphoinositide turnover in the human gastric cell line HGT1. J. Biol. Chem. 267, 25315-25320. 

Hatta, E, Imamura, M., Yasuda, K., Levi, R., 1996. Activation of histamine H3-receptors inhibits carrier-mediated norepinephrine release in a human model of protracted myocardial ischemia. Circulation 94,1-474. 

Ichinose, M., Barnes, P.J., 1989b. Inhibitory histamine H3-receptors on cholinergic nerves in human aiways. Eur. J. Pharmacol. 163, 383-386. 

Molderings, G.J., Weiflenborn, G., Schlicker, E., Likungu, J., Gothert, M., 1992. Inhibition of noradrenaline release from the sympathetic nerves of the human saphenous vein by presynaptic histamine H3 receptors. Naunyn-Schmiedeberg s Arch. Pharmacol. 346, 46-50. 

Imamura M, Seyedi N, Lander HM, Levi R (1995) Functional identification of histamine H3-receptors in the human heart. Circ Res 77 206-10 Imamura M, Smith NC, Garbarg M, Levi R (1996a) Histamine H3-receptor-mediated inhibition of calcitonin gene-related peptide release from cardiac C fibers. A regulatory negative-feedback loop. Circ Res 78 863-9... 

Koyama M, Heerdt PM, Levi R (2003) Increased severity of reperfusion arrhythmias in mouse hearts lacking histamine H3-receptors. Biochem Biophys Res Commun 306 792-6 Koyama S, Brodie MS, Appel SB (2007) Ethanol inhibition of M-current and ethanol-induced direct excitation of ventral tegmental area dopamine neurons. J Neurophysiol 97 1977-85 Kuzhikandathil EV, Yu W, Oxford GS (1998) Human dopamine D3 and D2l receptors couple to inward rectifier potassium channels in mammalian cell lines. Mol Cell Neurosci 12 390 102 Kuzhikandathil EV, Oxford GS (1999) Activation of human D3 dopamine receptor inhibits P/Q-type calcium channels and secretory activity in AtT-20 cells. J Neurosci 19 1698-1707... 

Schlicker E, Fink K, Detzner M, Gothert M (1993) Histamine inhibits dopamine release in the mouse striatum via presynaptic H3 receptors. J Neural Transm Gen Sect 93 1-10 Schlicker E, Kathmann M, Detzner M, Exner HJ, Gothert M (1994) H3 receptor-mediated inhibition of noradrenaline release an investigation into the involvement of Ca2+ and K+ ions, G protein and adenylate cyclase. Naunyn Schmiedeberg s Arch Pharmacol 350 34 11 Schlicker E, Werthwein S, Zentner J (1999) Histamine H3 receptor-mediated inhibition of noradrenaline release in the human brain. Fundam Clin Pharmacol 13 120-2 Schmitz D, Gloveli T, Empson RM, Draguhn A, Heinemann U (1998) Serotonin reduces synaptic excitation in the superficial medial entorhinal cortex of the rat via a presynaptic mechanism. J Physiol 508 119-29... 

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