Hl histamine receptor

Dopamine receptors are found in high concentration in the area postrema, which contains the chemoreceptor trigger zone (CTZ). Histamine Hl-receptors are concentrated in the nucleus tractus solitarius, which processes information relating to emesis, and in the dorsal motor nucleus of the vagus. This nucleus and the nucleus ambiguus also contain muscarinic cholinergic receptors, and these initiate motor components of vomiting. 

Introduction Histamine receptors Histamine Hl-receptor antagonists H 2-receptor antagonists INTRODUCTION... 

Recently a number of pharmaceutical drugs have been withdrawn from the market or not granted approval due to their pro-arrhythmic tendencies linked to inhibition of hERG. Two examples of this are terfenadine (Seldane) [91], a histamine Hl-receptor antagonist, and cisapride (Propulsid) [92], a gastric pro-kinetic. For this reason the safety assessment profile of any novel compound must now consider the IC50 value of the compound for hERG. 

Rotter A, Frostholm A (1986) Cerebellar histamine-Hl receptor distribution An autoradiographic study of Purkinje cell degeneration, staggerer, weaver and reeler mutant mouse strains. Brain Res. Bull, 16,205-214. 

Chang, R.S.L., Tran, V.T. and Snyder, S.H. (1979) Heterogenicity of histamine Hl-receptors species variations in [3H]mepyramine binding of brain membranes. J. Neurochem. 32 1653-1663. 

Ellman s auxiliary has also been used in Sepracor s synthesis of cetirizine 248 a histamine Hl-receptor agonist. Sulfinamide 244 was treated... 

Doreulee N, Yanovsky Y, Flagmeyer I, Stevens DR, Haas HL, Brown RE (2001) Histamine H3 receptors depress synaptic transmission in the corticostriatal pathway. Neuropharmacology 40 106-13... 

Honig P, Baraniuk JN. Adverse effects of Hl-receptor antagonists in the cardiovascular system. In Simons FER, editor. Histamine and Hl-receptor Antagonists in Allergic Disease. New York Marcel Dekker Inc, 1996 383 12. 

Meltzer, H.Y. and Roth, B.L. (2003) Hl-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychophurmacology, 28 (3),... 

Seifert, R., Hoer, A., Offermans, S., Buschauer, A., Schunack, W. (1992). Histamine increases cytosolic Ca2+ in dibutyryl-cAMP-differentiated HL-60 cells via H receptors and is an incomplete secretagogue. Am. Soc. Pharmacol. Exp. Therapeut. 

Seifert R, Hageluken A, Hoer A, Hoer D, Grunbaum L, Offermanns S, Schwaner I, Zinge V, Schunack W, Schultz G (1994) The HI receptor agonist 2-(3-chlorophenyl) histamine activates Gi proteins in HL-60 cells through a mechanism that is independent of known histamine receptor subtypes. Mol Pharmacol... 

Brookhuis KA, De Vries G, De Waard D. Acute and subchronic effects of the Hl-histamine receptor antagonist ebastine in 10, 20 and 30 mg dose, and triprolidine 10 mg on car driving performance. Br J Clin Pharmacol 1993 36 67-70. 

Hl-KO, H3-KO, histamine HI, H3 receptor gene double knockout (HI/H3-DKO), HI, H2, and H3 receptor gene triple knockout (TKO), and their WT mice were used in this study. The mice were bred in our laboratory (Sakurai et al., 2008). All experiments were performed in accordance with institutional guidelines, and experimental protocols were approved by the Animal Care Committee of Tohoku University. 

From the study of the locomotor measurement, it is suggested that the histamine HI, H2, and H3 receptors might not play a decisive role in suppressing the behavioral sensitization. As for rewarding effects, Hl-KO mice showed the enhanced rewarding behaviors, while H3-KO mice exhibited the suppressive CPP responses. These data suggest that HI receptor might have an important role to prevent METH-induced reward effects. 

Nicholson AN, Stone BM. Performance studies with the Hl-histamine receptor antagonists, astemizole and ter-fenadine. Br J Chn Pharmacol 1982 13(2) 199-202. 

Lipp R, Stark H, Schunack W. In Schwartz JC, Haas HL, eds. The Histamine Receptor. New York Wiley-Liss, Inc., 1992 57-72. 

Whereas Hi receptors are involved with positive effects, H2 receptors appear to mainly mediate suppressive activities of histamine including gastric acid secretion, heart contraction, cell proliferation, differentiation, and some effects on the immune response. H2 receptors are coupled to the adenylate cyclase as well as the phosphoinositide second messenger systems via separate GTP-dependent mechanisms, but H2-dependent effects, particularly those of the central nervous system, are predominantly mediated through cAMP. It has been shown that receptor binding stimulates activation of c-Fos, c-Jun, PKC, and P70S6 kinase. Alternative signaling pathways have been reported (Fig. 3.7). These include a receptor-mediated increase in intracellular Ca and/or IP3 levels in HL-60 human promyelocytic leukemia cells and an increase in cAMP and inhibition of release of arachidonic acid in Chinese hamster ovary (CHO) cells transfected with rat cDNA and induced by calcium ionophore. 

Klimek L. Levocetirizine from scientific evidence to a potent modern-day treatment of today s allergic patients. Drugs Today 2009 45(3) 213-25. Gillard M, Van Der Perren C, Moguilevsky N, Massingham R, Chatelain P. Binding characteristics of cefirizine and levocetirizine to human Hl-histamine receptors. Mol Pharmacol 2002 61 391-9. 

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