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Substituent Effect in Histamine and Its Impact on Interactions with the G Protein-Coupled Human Receptor H₁ Modelled by Quantum-Chemical Methods. [PDF]

Molecules
Jezuita A, Makowska-Janusik M, Ejsmont K, Marczak W.   +3 more
europepmc   +1 more source

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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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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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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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Homologous histamine H1 receptor desensitization results in reduction of H1 receptor agonist efficacy

European Journal of Pharmacology, 1991
Prolonged exposure of the guinea-pig intestinal longitudinal smooth muscle to histamine caused homologous desensitization of the H1 receptor, which led to reduced H1 receptor-mediated production of [3H]inositol phosphates as well as to reduced H1 agonist-induced contractions.
Leurs, R, Smit, M J, Bast, A, Timmerman, H   +3 more
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Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines

Inflammation Research, 2005
The predictive efficacy of drugs in humans is frequently estimated from both a high affinity for their receptor as measured in vitro and a long plasmatic half-life. This is grossly misleading since one key parameter is missing: drug concentration at the receptor site in vivo.
M, Gillard, M Strolin, Benedetti, P, Chatelain, E, Baltes   +3 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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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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Pharmacokinetic Optimisation of Histamine H1-Receptor Antagonist Therapy

Clinical Pharmacokinetics, 1991
Second-generation, relatively nonsedating histamine H1-receptor antagonists (H1-RA) are extensively used worldwide for the symptomatic treatment of allergic rhinoconjunctivitis and chronic urticaria. Information about the pharmacokinetics and pharmacodynamics of these medications, while still incomplete, is now sufficient to permit optimisation of ...
F. Estelle, R. Simons, Keith J. Simons
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