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Antihistaminergics and inverse agonism. Potential therapeutic applications
(Elsevier, 2013-09)
The accurate characterization of the molecular mechanisms involved in the action of receptor ligands is important for their appropriate therapeutic use and safety. It is well established that ligands acting at the histamine ...
Extracellular Signaling Receptors
(Springer, 2009)
Classically, receptors were defined as cellular structures that recognize and bind hormones. In present days this definition is expanded to include receptors for a variety of other extracellular regulatory signaling ...
Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein
(American Society for Biochemistry and Molecular Biology, 2004)
Accurate characterization of the molecular mechanisms of the action of ligands is an extremely important issue for their appropriate research, pharmacological, and therapeutic uses. In view of this fact, the aim of the ...
Fluorinated oxysterol analogues: Synthesis, molecular modelling and liver X receptor activity
(Pergamon-Elsevier Science Ltd, 2017)
Liver X receptors (LXRs) are nuclear receptors that play central roles in the transcriptional control of lipid metabolism. They also modulate immune and inflammation responses in macrophagues and have multiple roles in ...
Behavioral differences between subgroups of rats with high and low threshold to clonic convulsions induced by DMCM, a benzodiazepine inverse agonist
(Elsevier B.V., 2005-11-01)
In epileptic patients, there is a high incidence of psychiatric comorbidities, such as anxiety. Gamma-aminobutyric acid (GABA) ionotropic receptor GABA(A)/benzodiazepine allosteric site is involved in both epilepsy and ...
Anxiogenic-like Effects Induced By Hemopressin In Rats
(PERGAMON-ELSEVIER SCIENCE LTDOXFORD, 2015)
Development of a novel fluorescent ligand of growth hormone secretagogue receptor based on the N-Terminal Leap2 region
(Elsevier Ireland, 2019-12-01)
Liver-expressed antimicrobial peptide 2 (LEAP2) was recently recognized as an endogenous ligand for the growth hormone secretagogue receptor (GHSR), which also is a receptor for the hormone ghrelin. LEAP2 blocks ghrelin-induced ...
Inflammation triggers constitutive activity and agonist-induced negative responses at M(3) muscarinic receptor in dental pulp
(Elsevier Science Inc, 2011-02)
The purpose of this study was to investigate whether the inflammation of rat dental pulp induces the muscarinic acetylcholine receptor (mAChR) constitutive receptor activity. Pulpitis was induced with bacterial lipolysaccharide ...