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 …
Its physiological functions are mediated by four 7-transmembrane G protein–coupled …
The roles of histamine and its receptor ligands in central nervous system disorders: An update
W Hu, Z Chen - Pharmacology & therapeutics, 2017 - Elsevier
The neurotransmitter histamine receives less attention compared with other biogenic
amines, because of its moderate action in the central nervous system (CNS). However …
amines, because of its moderate action in the central nervous system (CNS). However …
Biased agonism in drug discovery—is it too soon to choose a path?
MC Michel, SJ Charlton - Molecular pharmacology, 2018 - ASPET
A single receptor can activate multiple signaling pathways that have distinct or even
opposite effects on cell function. Biased agonists stabilize receptor conformations …
opposite effects on cell function. Biased agonists stabilize receptor conformations …
Histamine H1, H3 and H4 receptors are involved in pruritus
K Rossbach, C Nassenstein, M Gschwandtner… - Neuroscience, 2011 - Elsevier
Histamine has long been recognised as a classical inducer of pruritus. However, the specific
mechanism of histamine-induced itch has still not been fully understood. The H1 and H4 …
mechanism of histamine-induced itch has still not been fully understood. The H1 and H4 …
Inhibitors of membranous adenylyl cyclases
R Seifert, GH Lushington, TC Mou, A Gille… - Trends in …, 2012 - cell.com
Membranous adenylyl cyclases (mACs) constitute a family of nine isoforms with different
expression patterns. Studies with mAC gene knockout mice provide evidence for the notion …
expression patterns. Studies with mAC gene knockout mice provide evidence for the notion …
Cherry-picked ligands at histamine receptor subtypes
Histamine, a biogenic amine, is considered as a principle mediator of multiple physiological
effects through binding to its H 1, H 2, H 3, and H 4 receptors (H1–H4Rs). Currently, the HRs …
effects through binding to its H 1, H 2, H 3, and H 4 receptors (H1–H4Rs). Currently, the HRs …
Synthesis, biological evaluation, and computational studies of Tri-and tetracyclic nitrogen-bridgehead compounds as potent dual-acting AChE inhibitors and h H3 …
Combination of AChE inhibiting and histamine H3 receptor antagonizing properties in a
single molecule might show synergistic effects to improve cognitive deficits in Alzheimer's …
single molecule might show synergistic effects to improve cognitive deficits in Alzheimer's …
Paradoxical stimulatory effects of the “standard” histamine H4-receptor antagonist JNJ7777120: the H4 receptor joins the club of 7 transmembrane domain receptors …
R Seifert, EH Schneider, S Dove, I Brunskole… - Molecular …, 2011 - ASPET
The histamine H4 receptor (H4R) is expressed in several cell types of the immune system
and is assumed to play an important pro-inflammatory role in various diseases, including …
and is assumed to play an important pro-inflammatory role in various diseases, including …
Species-dependent activities of G-protein-coupled receptor ligands: lessons from histamine receptor orthologs
A Strasser, HJ Wittmann, A Buschauer… - Trends in …, 2013 - cell.com
Histamine is a biogenic amine that exerts its biological effects as a neurotransmitter and
local mediator via four histamine receptor (HR) subtypes (H x Rs)–H 1 R, H 2 R, H 3 R, and …
local mediator via four histamine receptor (HR) subtypes (H x Rs)–H 1 R, H 2 R, H 3 R, and …
Incomplete activation of human eosinophils via the histamine H4-receptor: evidence for ligand-specific receptor conformations
TM Reher, D Neumann, A Buschauer… - Biochemical pharmacology, 2012 - Elsevier
Eosinophils play a crucial role in the pathogenesis of allergic diseases. Histamine activates
eosinophils via the H4-receptor (H4R). However, pharmacological analysis of the H4R in …
eosinophils via the H4-receptor (H4R). However, pharmacological analysis of the H4R in …