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 …

Histamine in the nervous system

HL Haas, OA Sergeeva, O Selbach - Physiological reviews, 2008 - journals.physiology.org
Histamine is a transmitter in the nervous system and a signaling molecule in the gut, the
skin, and the immune system. Histaminergic neurons in mammalian brain are located …

Regulation of the immune response and inflammation by histamine and histamine receptors

L O'Mahony, M Akdis, CA Akdis - Journal of Allergy and Clinical …, 2011 - Elsevier
Histamine is a biogenic amine with extensive effects on many cell types, including important
immunologic cells, such as antigen-presenting cells, natural killer cells, epithelial cells, and …

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 …

The evasive nature of drug efficacy: implications for drug discovery

S Galandrin, G Oligny-Longpré, M Bouvier - Trends in pharmacological …, 2007 - cell.com
The efficacy of a drug is generally determined by the drug's ability to promote a quantifiable
biological response. In the context of the classical receptor-occupancy theory, the efficacy is …

Distinct signaling profiles of β1 and β2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of …

S Galandrin, M Bouvier - Molecular pharmacology, 2006 - ASPET
Drug efficacy is typically considered an intrinsic property of a ligand/receptor couple.
However, recent observations suggest that efficacy may also be influenced by the signaling …

Histamine receptors in the CNS as targets for therapeutic intervention

MB Passani, P Blandina - Trends in pharmacological sciences, 2011 - cell.com
Histamine has long been known to trigger allergic reactions and gastric acid secretion.
However, it was later discovered that, in the brain, histamine regulates basic homeostatic …

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 …

G‐protein‐coupled receptors: past, present and future

SJ Hill - British journal of pharmacology, 2006 - Wiley Online Library
The G‐protein‐coupled receptor (GPCR) family represents the largest and most versatile
group of cell surface receptors. Drugs active at these receptors have therapeutic actions …

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) …