Results 41 to 50 of about 19,980 (209)

Histamine and Histamine H4 Receptor Promotes Osteoclastogenesis in Rheumatoid Arthritis. [PDF]

open access: yes, 2017
Histamine H4 receptor (H4R) has immune-modulatory and chemotaxic effects in various immune cells. This study aimed to determine the osteoclastogenic role of H4R in rheumatoid arthritis (RA).
Firestein, Gary S   +5 more
core   +1 more source

Neuropharmacological targets for drug action in vestibular sensory pathways [PDF]

open access: yes, 2017
The use of pharmacological agents is often the preferred approach to the management of vestibular dysfunction. In the vestibular sensory pathways, the sensory neuroepithelia are thought to be influenced by a diverse number of neuroactive substances that ...
Jones, Timothy A, Lee, Choongheon
core   +3 more sources

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

open access: yes, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie   +3 more
core   +1 more source

Prodrugs Activated by Vascular Ectopeptidases: Proof of Concept

open access: yesMedical Sciences Forum, 2022
Several vascular ectopeptidases reside in blood vessels and efficiently regulate peptide hormones. For instance, bradykinin (BK) is inactivated by angiotensin converting enzyme (ACE) or arginine-carboxypeptidases (Arg-CPs), and aminopeptidase N (APN ...
François Marceau
doaj   +1 more source

Influence of mirtazapine on salivary cortisol in depressed patients [PDF]

open access: yes, 2003
Unlike other antidepressants, mirtazapine does not inhibit the reuptake of norepinephrine or serotonin but acts as an antagonist at presynaptic alpha(2)-receptors, at postsynaptic 5-HT2 and 5-HT3 receptors, and at histaminergic H1 receptors. Furthermore,
Baghai, Thomas C.   +3 more
core   +1 more source

Proteomic Profiling Informs Mechanisms of Esophageal Adenocarcinoma Inhibition by Cranberry Proanthocyanidins

open access: yesMolecular Nutrition &Food Research, EarlyView.
In this study we utilized proteomic profiling to investigate mechanisms linked to the cancer‐inhibitory effect of cranberry proanthocyanidins (CPACs) on reflux‐induced esophageal adenocarcinoma in a rat model. The results indicate that CPAC inhibits cancer through targeting multiple hallmarks of cancer known to be dysregulated in progression to ...
Yun Zhang   +7 more
wiley   +1 more source

Plasticity of histamine H3 receptor expression and binding in the vestibular nuclei after labyrinthectomy in rat [PDF]

open access: yes, 2004
Background: In rat, deafferentation of one labyrinth (unilateral labyrinthectomy) results in a characteristic syndrome of ocular and motor postural disorders (e.g., barrel rotation, circling behavior, and spontaneous nystagmus). Behavioral recovery (e.g.,
Aarnisalo, Antti A.   +4 more
core   +2 more sources

AI‐Driven Identification of Exceptionally Efficacious Polypharmacological Compounds That Extend the Lifespan of Caenorhabditis elegans

open access: yesAging Cell, EarlyView.
A retrospective analysis of the most effective known geroprotectors shows that they act by polypharmacological mechanisms. Using graph neural networks, we predict polypharmacological geroprotectors, validate their polypharmacological mechanisms experimentally, and show them to be exceptionally effective.
Konstantin Avchaciov   +5 more
wiley   +1 more source

Votucalis, a Novel Centrally Sparing Histamine-Binding Protein, Attenuates Histaminergic Itch and Neuropathic Pain in Mice

open access: yesFrontiers in Pharmacology, 2022
Votucalis is a biologically active protein in tick (R. appendiculatus) saliva, which specifically binds histamine with high affinity and, therefore, has the potential to inhibit the host’s immunological responses at the feeding site. We hypothesized that
Ibrahim Alrashdi   +12 more
doaj   +1 more source

ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

open access: yesBritish Journal of Pharmacology, EarlyView.
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

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