Results 191 to 200 of about 696,707 (241)

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

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
openaire   +2 more sources

Histamine H1- and H2-receptors in the gastrointestinal circulation

Naunyn-Schmiedeberg's Archives of Pharmacology, 1980
Evidence for the presence of specific histamine H1- and H2-receptors in the gastrointestinal circulation was obtained using histamine, 2-methylhistamine (a specific H1-agonist), 4-methylhistamine (a specific H2-agonist), and selective H1- and H2-receptor antagonists in the anesthetized dog.
G A, Charbon, H A, Brouwers, A, Sala
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

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
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

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
openaire   +2 more sources

Interactions of Histamine H1-Receptor Agonists and Antagonists with the Human Histamine H4-Receptor

Molecular Pharmacology, 2009
The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H(1)R ligands bind to hH(4)R.
Karl-Friedrich, Deml, Silke, Beermann, Detlef, Neumann, Andrea, Strasser, Roland, Seifert   +4 more
openaire   +2 more sources

The histamine H1‐receptor mediates the motivational effects of novelty

European Journal of Neuroscience, 2008
AbstractNovelty‐induced arousal has motivational effects and can reinforce behavior. The mechanisms by which novelty acts as a reinforcer are unknown. Novelty‐induced arousal can be either rewarding or aversive dependent on its intensity and the preceding state of arousal.
ZLOMUZICA A., VIGGIANO D., DE SOUZA SILVA M., ISHIZUKA T., GIRONI U., CARNEVALE U., RUOCCO L. A., WATANABE T., SADILE, Adolfo, . HUSTON J., DERE E.   +10 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