Results 191 to 200 of about 12,014 (244)

Domain Swapping in the Human Histamine H1 Receptor

The Journal of Pharmacology and Experimental Therapeutics, 2004
G-protein-coupled receptors (GPCRs) represent the largest family of receptors involved in transmembrane signaling. Although these receptors were generally believed to be monomeric entities, accumulating evidence supports the presence of GPCRs in multimeric forms.
Bakker, R.A., Dees, G., Carrillo, J.J., Booth, R.G., Lopez-Gimenez, J.F., Milligan, G., Strange, P.G., Leurs, R.   +7 more
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Structural Analysis of the Histamine H1 Receptor

2016
The 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.
Mitsunori, Shiroishi, Takuya, Kobayashi
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Developments in histamine H1-receptor agonists

1995
The story of histamine started in the early 1900’s with the fundamental investigations of Dale et al. [l–3], which recognized the remarkable physiological behavior of this biogenic amine. Scientific progress over the past decades has proved that histamine interacts with specific histamine receptors as a neurotransmitter and nearly all mammalian tissues
V, Zingel, C, Leschke, W, Schunack
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Characterization of vascular histamine H1-receptors: Multiple affinity states of aortic histamine H1-receptor

Agents and Actions, 1985
We have shown that [3H]mepyramine labels histamine H1-receptor-binding sites in bovine aortic membranes. Further characterization of H1-receptors in this tissue was done by the interaction of an unlabelled histamine receptor agonist or antagonist, with the radioantagonist [3H]mepyramine-binding sites.
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Characteristics of histamine H1 receptors on HeLa cells

European Journal of Pharmacology: Molecular Pharmacology, 1993
The 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 A, Arias-Montaño, J M, Young
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Structural elements of H1- and H2-receptors of histamine

General Pharmacology: The Vascular System, 1980
Abstract 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 L, Grechishkin, V L, Goldfarb, L K, Gavrovskaya, N B, Brovtsyna   +3 more
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Histamine H1 and H2-Receptors at a Ganglionic Synapse

Nature, 1973
MANY humoral agents are capable of modulating synaptic transmission in sympathetic ganglia and it has been proposed that a variety of receptors are present at the ganglionic synapse (see Haefely1). There are thus many possible modulatory mechanisms at this synapse, some of which have a dual nature, the same substance being able both to facilitate and ...
M J, Brimble, D I, Wallis
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Conformationally-restricted ligands for the histamine H1 receptor

Bioorganic & Medicinal Chemistry Letters, 2000
Potent H1-antagonistic activity in a series of novel indeno[2,1-c]pyridines and their 4-arylpiperidinol precursors is reported; one compound shows an in vitro activity four times that of the standard mepyramine that it was screened against. Their failure to translate this protection to in vivo tests is discussed.
C, Upton, R H, Osborne, M, Jaffar
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Histamine H1 receptors in the CNS

Trends in Pharmacological Sciences, 1979
Abstract 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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Histamine H1-receptor in the retina: Species differences

Biochemical and Biophysical Research Communications, 1988
Histamine H1-receptors in membranes of the various mammalian retinas were studied by [3H]mepyramine binding assay. Specific [3H]mepyramine bindings to bovine, pig, dog and human retinas were observed with the dissociation constants (KD), 3.8 +/- 1.2 nM, 1.8 +/- 0.6 nM, 2.6 +/- 0.6 nM and 3.0 +/- 0.9 nM, respectively, which were similar to those found ...
S, Sawai, N P, Wang, H, Fukui, M, Fukuda, R, Manabe, H, Wada   +5 more
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