Cytokine responses of intraepithelial lymphocytes are regulated by histamine H2 receptor [PDF]
Backgrounds. Histamine participates in the immune regulation of several gastrointestinal diseases. However, the effect of histamine on intestinal intraepithelial lymphocytes (IELs), the front line of intestinal mucosal immune system, is not well ...
A Di Sabatino+58 more
core +1 more source
ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison+15 more
wiley +1 more source
Purpose: Fexofenadine (FXF) is the active metabolite of terfenadine with selective peripheral H1 receptor antagonist activity. FXF is a third-generation antihistamine, non-sedating, rapid and very long acting used in symptoms associated with allergic ...
Natalia Kordulewska+4 more
doaj +1 more source
The impact of high density receptor clusters on VEGF signaling [PDF]
Vascular endothelial growth factor (VEGF) signaling is involved in the process of blood vessel development and maintenance. Signaling is initiated by binding of the bivalent VEGF ligand to the membrane-bound receptors (VEGFR), which in turn stimulates receptor dimerization.
arxiv +1 more source
Association of genetic variants of the histamine H1 and muscarinic M3 receptors with BMI and HbA1c values in patients on antipsychotic medication [PDF]
Rationale: Antipsychotic affinity for the histamine H1 receptor and the muscarinic M3 receptor have been associated with the side effects weight gain, and development of diabetes, respectively.
A Matsui-Sakata+60 more
core +5 more sources
Progress on the development of Class A GPCR‐biased ligands
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales+20 more
wiley +1 more source
In vitro H1-receptor antagonist activity of methanolic extract of tuber of Stephania glabra
In the present study, methanolic extract of tuber of Stephania glabra was evaluated for H1-bloker activity by employing in vitro screening models of guinea pig ileum and goat tracheal chain preparation.
Nisar Ahmad Khan+5 more
doaj +1 more source
Histaminergic H3-Heteroreceptors as a Potential Mediator of Betahistine-Induced Increase in Cochlear Blood Flow [PDF]
OBJECTIVE Betahistine is a histamine-like drug that is considered beneficial in Ménière's disease by increasing cochlear blood flow. Acting as an agonist at the histamine H1-receptor and as an inverse agonist at the H3-receptor, these receptors as well ...
Bertlich, Mattis+5 more
core +1 more source
A Thermodynamic Model for Receptor Clustering [PDF]
Intracellular signaling often arises from ligand-induced oligomerization of cell surface receptors. This oligomerization or clustering process is fundamentally a cooperative behavior between near-neighbor receptor molecules; the properties of this cooperative process clearly affects the signal transduction.
arxiv +1 more source
High- and low-conductance NMDA receptors are present in layer 4 spiny stellate and layer 2/3 pyramidal neurons of mouse barrel cortex [PDF]
NMDA receptors are ion channels activated by the neurotransmitter glutamate in the mammalian brain and are important in synaptic function and plasticity, but are also found in extrasynaptic locations and influence neuronal excitability. There are different NMDA receptor subtypes which differ in their single-channel conductance.
arxiv +1 more source