Results 141 to 150 of about 10,364 (172)

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
openaire   +3 more sources

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
openaire   +2 more sources

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
openaire   +2 more sources

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
openaire   +2 more sources

Chlorpheniramine plasma concentration and histamine H1-receptor occupancy*

Clinical Pharmacology & Therapeutics, 1995
The plasma concentration-response relationship of the antihistamine chlorpheniramine is poorly characterized. This study examined concurrently the concentrations of chlorpheniramine and presence of H1-receptor antagonist in plasma after administration of 8 mg chlorpheniramine in normal volunteers.
S U, Yasuda, A, Wellstein, P, Likhari, J T, Barbey, R L, Woosley   +4 more
openaire   +2 more sources

The roles of histamine H1 receptors on cognition

Inflammation Research, 2008
Histamine neurons are located exclusively in the posterior hypothalamus, from where they project diffusely to all regions of brain. Neuronal histamine has been implicated in a variety of brain functions including wakefulness, learning and memory [1].
K, Yanai, H, Dai, E, Sakurai, T, Watanabe   +3 more
openaire   +2 more sources

Genomic Cloning of the Rat Histamine H1 Receptor

Biochemical and Biophysical Research Communications, 1993
A 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 ...
K, Fujimoto, Y, Horio, K, Sugama, S, Ito, Y Q, Liu, H, Fukui   +5 more
openaire   +2 more sources

Interactions between adenosine A1- and histamine H1-receptors

International Journal of Biochemistry, 1994
The interactions or "cross-talk" between adenosine A1-receptors and receptors coupled to phospholipase C (leading to the hydrolysis of inositol phospholipids) have been well documented in the literature. For example, activating the A1-receptor selectively potentiates the histamine H1-receptor stimulated hydrolysis of inositol phospholipids in guinea ...
J M, Dickenson, S J, Hill
openaire   +2 more sources

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.
openaire   +1 more source