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Structural Analysis of the Histamine H1 Receptor
2016The crystal structure of the human histamine H1 receptor (H1R) has been determined in complex with its inverse agonist doxepin, a first-generation antihistamine. The crystal structure showed that doxepin sits deeply inside the ligand-binding pocket and predominantly interacts with residues highly conserved among other aminergic receptors.
Takuya Kobayashi, Mitsunori Shiroishi
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Histamine H1 receptors in the CNS
Trends in Pharmacological Sciences, 1979Abstract Despite the explosion of activity in the receptor labelling field in recent years, the histamine H 1 receptor has been surprisingly neglected. The synthesis of a suitable H-ligand has filled this gap and provided the means to obtain information on the properties and distribution of histamine H 1 receptors in the CNS.
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Molecular modeling of the histamine H1 receptor
[1992] Proceedings of the Eighteenth IEEE Annual Northeast Bioengineering Conference, 2003Summary form only given. The authors review the properties and functional characteristics of the H/sub 1/ receptor and postulate the nature of the ligand-receptor activation site using molecular modeling techniques. A model of the surface of the active site on the receptor was postulated and constructed using Sybyl software on a personal Iris ...
Arthur B. Ritter +3 more
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Structural elements of H1- and H2-receptors of histamine
General Pharmacology: The Vascular System, 1980Abstract This article sets out the proposed schemes of histamine H 1 - and H 2 -receptors. These schemes are based on the analysis of histamine agonists activity.
L.K. Gavrovskaya +3 more
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Characteristics of histamine H1 receptors on HeLa cells
European Journal of Pharmacology: Molecular Pharmacology, 1993The affinities of antagonists at histamine H1 receptors on HeLa cells have been determined from inhibition of histamine-induced inositol phosphate formation in intact and from inhibition of [3H]mepyramine binding to HeLa cell membranes. The dissociation constants of mepyramine and (+)-chlorpheniramine were similar to values for binding to H1 receptors ...
J. Michael Young +1 more
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Biochemical and Biophysical Research Communications - BBRC, 1994
Based on structural comparison with other biogenic amine receptors and the histamine H2 receptor, it has been suggested that in the human histamine H1 receptor, Asp107, Thr194, and Asn198 are the residues involved in binding of histamine.
Kazumi Ohta +5 more
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Based on structural comparison with other biogenic amine receptors and the histamine H2 receptor, it has been suggested that in the human histamine H1 receptor, Asp107, Thr194, and Asn198 are the residues involved in binding of histamine.
Kazumi Ohta +5 more
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Genomic Cloning of the Rat Histamine H1 Receptor
Biochemical and Biophysical Research Communications, 1993A rat histamine H1 receptor gene which lacked introns was isolated from a rat genomic library using recently cloned bovine histamine H1 receptor cDNA [Yamashita et al., Proc. Natl. Acad. Sci. USA, 88, 11515-11519 (1991)]. The receptor protein deduced from this isolated gene was composed of 486 amino acids and showed characteristic properties of G ...
Hiroyuki Fukui +5 more
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Journal of Separation Science, 2014
Allergy is an abnormal reaction of the body to an allergen. Histamine is responsible for many of the acute symptoms of allergic diseases. Many of the allergic and inflammatory actions of histamine are mediated by the histamine H1 receptor. In the present
Ying-ying Guo +4 more
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Allergy is an abnormal reaction of the body to an allergen. Histamine is responsible for many of the acute symptoms of allergic diseases. Many of the allergic and inflammatory actions of histamine are mediated by the histamine H1 receptor. In the present
Ying-ying Guo +4 more
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Circulation Research, 1995
We compared the cardiac electrophysiological actions of two types of H1-receptor antagonists--the piperidines, astemizole and terfenadine, and the nonpiperidines, chlorpheniramine and pyrilamine-in vitro in guinea pig ventricular myocytes and in vivo in ...
J. Salata +5 more
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We compared the cardiac electrophysiological actions of two types of H1-receptor antagonists--the piperidines, astemizole and terfenadine, and the nonpiperidines, chlorpheniramine and pyrilamine-in vitro in guinea pig ventricular myocytes and in vivo in ...
J. Salata +5 more
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Molecular cloning of the human histamine H1 receptor gene.
Biochemical and Biophysical Research Communications - BBRC, 1994The human histamine H1 receptor gene, an intron-lacking gene, was isolated with bovine H1 receptor cDNA [Yamashita, M., Fukui, H., Sugama, K., Horio, Y., Ito, S., Mizuguchi, H., and Wada, H. (1991) Proc. Natl. Acad. Sci.
Hiroyuki Fukui +7 more
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