International union of basic and clinical pharmacology. XCVIII. Histamine receptors

P Panula, PL Chazot, M Cowart, R Gutzmer… - Pharmacological …, 2015 - ASPET
Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues.
Its physiological functions are mediated by four 7-transmembrane G protein–coupled …

The histamine H3 receptor: structure, pharmacology, and function

G Nieto-Alamilla, R Márquez-Gómez… - Molecular …, 2016 - ASPET
Among the four G protein–coupled receptors (H1–H4) identified as mediators of the biologic
effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclusive …

Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors

R Seifert, K Wenzel-Seifert - Naunyn-Schmiedeberg's archives of …, 2002 - Springer
The aim of this review is to provide a systematic overview on constitutively active G-protein-
coupled receptors (GPCRs), a rapidly evolving area in signal transduction research. We will …

Principles: receptor theory in pharmacology

T Kenakin - Trends in pharmacological sciences, 2004 - cell.com
Pharmacological receptor theory is discussed with special reference to advances made
during the past 25 years. Thus, the operational model has supplanted analysis of drug …

The histamine H3 receptor: from gene cloning to H3 receptor drugs

R Leurs, RA Bakker, H Timmerman… - Nature reviews Drug …, 2005 - nature.com
Since the cloning of the histamine H3 receptor cDNA in 1999 by Lovenberg and co-workers,
this histamine receptor has gained the interest of many pharmaceutical companies as a …

Histamine in the regulation of wakefulness

MM Thakkar - Sleep medicine reviews, 2011 - Elsevier
The histaminergic system is exclusively localized within the posterior hypothalamus with
projection to almost all the major regions of the central nervous system. Strong and …

The [35S] GTPγS binding assay: approaches and applications in pharmacology

C Harrison, JR Traynor - Life sciences, 2003 - Elsevier
Receptors of the of seven transmembrane spanning, heterotrimeric G protein coupled family
(GPCR) play crucial roles in regulating physiological functions and consequently are targets …

The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders

MB Passani, JS Lin, A Hancock, S Crochet… - Trends in …, 2004 - cell.com
Histamine H 3 receptor pharmacology, functions and biochemistry are far from being fully
understood; however, progress is being made. Activation of this G i/G o-protein-coupled …

Trends in histamine research: new functions during immune responses and hematopoiesis

E Schneider, M Rolli-Derkinderen, M Arock… - TRENDS in Immunology, 2002 - cell.com
Histamine is a bioamine with multiple physiological activities. In the immune system, it not
only mediates the deleterious effects accompanying allergic reactions, but it acts also in a …

BF2. 649 [1-{3-[3-(4-Chlorophenyl) propoxy] propyl} piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor …

X Ligneau, D Perrin, L Landais, JC Camelin… - … of Pharmacology and …, 2007 - ASPET
Histamine H3 receptor inverse agonists are known to enhance the activity of histaminergic
neurons in brain and thereby promote vigilance and cognition. 1-{3-[3-(4-Chlorophenyl) …