Histamine H3 receptor antagonists

Ligneau, X., Lin, J., Vanni-Mercier, G. et at (1998). Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J. Pharmacol. 

Munzar, R, Tanda, G., Justinova, Z., Goldberg, S.R. Histamine h3 receptor antagonists potentiate methamphetamine self-administration and methamphetamine-induced accumbal dopamine release. Neuropsychopharmacology. 29 705, 2004. 

De Esch IJP, Mills JEJ, Perkins TDJ, Romeo G, Hoffmann M, Wieland K, Leurs R, Menge WMPB, Nederkoorn PHJ, Dean PM, Timmerman H. Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE. J Med Chem 2001 44 1666-1674. 

Witkin JM, Nelson DL. Selective histamine H3 receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous system. Pharmacol Ther 2004 103 1-20. 

S. Celanire, M. Wijtmans, P. Talaga, R. Leurs, I.J. de Esch, Keynote review Histamine H3 receptor antagonists reach out for the clinic, Dmg Discov. Today 10(2005) 1613-1627. 

Stark, H. Krause, M. Arrang, J.-M. Ligneau, X. Schwartz, J.-C. Schunack, W. Unsymmetrically Substituted Guanidines as Potent Histamine H3-Receptor Antagonists, Bioorg. Med. Chem. Lett. 1994, 4, 2907-2912. 

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, Schlicker E, Schunack W (1996) Developments of histamine H3-receptor antagonists. Drugs Future 21 507-520. 

Activities of some histamine H3 receptor antagonists on various in vitro functional models of the guinea pig intestine... 

Corbel, S., Traiffort, E., Stark, H., Schunack, W., Dy, M., 1997. Binding of histamine H3-receptor antagonists to hematopoietic progenitor cells. FEBS Letters 404, 289-293... 

Jansen, F.P., Rademaker, B., Bast, A. and Timmerman, H. (1992). The first radiolabelled histamine H3-receptor antagonist, [125i]iodophenpropit saturable and reversible binding to rat cortex membranes. Eur. J. Pharmacol. 217, 203-205. 

Since the disclosure of thioperamide 1 (K = 4 nM) as a potent and selective histamine H3 receptor antagonist [1], there has been a large number of 4(5)-substituted imidazole derivatives prepared and evaluated for their H3 receptor affinity. Most of the efforts directed towards the design of new H3 antagonists have... 

These data suggest that the contribution of the cholinergic system to the ameliorating effect induced by histamine H3-receptor antagonists is not mediated by histamine H3 hetero receptors, but by postsynaptic histamine H, receptors. This is supported by previous reports that histamine excites cholinergic neurons through histamine H, receptors [30, 31]. 

Fig. 5.6 Part of the pseudoreceptor model for histamine H3-receptor antagonists [25] (one leucine beside the isoleucine residue is omitted for clarity). Hydrogen bonds from ligands to complementary functions of asparagine (Asn), tyrosine (Tyr) and aspartate (Asp) are located in the GR/D-...

Wu SY, Wang MY, Dun NJ (1991) Serotonin via presynaptic 5-HTi receptors attenuates synaptic transmission to immature rat motoneurons in vitro. Brain Res 554 111-21 Yamamoto Y, Mochizuki T, Okakura-Mochizuki K, Uno A, Yamatodani A (1997) Thioperamide, a histamine H3 receptor antagonist, increases GABA release from the rat hypothalamus. Methods Find Exp Clin Pharmacol 19 289-98... 

Yokoo H, Goldstein M, Meller E (1988) Receptor reserve at striatal dopamine receptors modulating the release of [3H] dopamine. Eur J Pharmacol 155 323-7 Yokoyama H, Onodera K, Maeyama K, Sakurai E, Iinuma K, Leurs R, Timmerman H, Watanabe T (1994) Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur J Pharmacol 260 23-8 Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006) Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus. Proc Natl Acad Sci USA, in press Young CS, Mason R, Hill SJ (1988) Studies on the mechanism of histamine-induced release of noradrenaline and 5-hydroxytryptamine from slices of rat cerebral cortex. Biochem Pharmacol 37 2799-2805... 

Histamine receptors are related to skin barrier function.44 Three different types of histamine receptors, HI, H2, and H3 have been reported. First, topical application of histamine HI and H2 receptor antagonists accelerated the barrier repair. Histamine itself, H2 receptor agonist, and histamine releaser delayed the barrier repair. Histamine H3 receptor antagonist and agonist did not affect the barrier recovery rate. Topical application of the HI and H2 receptor antagonists prevented the epidermal hyperplasia induced by barrier disruption under low humidity. The mechanism of the relationship between the histamine receptors and the barrier repair process has not been elucidated yet. 

Esbenshade TA, Fox GB, Cowart MD. 2006. Histamine H3 receptor antagonists Preclinical promise for treating obesity and cognitive disorders. Mol Interv 6 77-88, 59. 

Antihistamines and Histamine H3 receptor antagonists and inverse agonists GSK239512 Latrepirdine (Dimebon)... 

Nathan PJ, Boardley R, Scott N, Berges A, Maruff P, Sivananthan T et al (2013) The safety, tolerability, pharmacokinetics and cognitive effects of GSK239512, a selective histamine H3 receptor antagonist in patients with mild to moderate Alzheimer s disease A preliminary investigation. Curr Alzheimer Res 10 240-251... 

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