SAR exploration of the non‐imidazole histamine H3 receptor ligand ZEL‐H16 reveals potent inverse agonism
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200451
Abstract: Histamine H3 receptor (H3R) agonists without an imidazole moiety remain very scarce. Of these, ZEL‐H16 (1) has been reported previously as a high‐affinity non‐imidazole H3R (partial) agonist. Our structure‐activity relationship analysis using derivatives of 1… read more here.
Keywords: inverse agonism; zel h16; agonism; non imidazole ... See more keywords
Histamine H1 receptor gene polymorphism acts as a biological indicator of the prediction of therapeutic efficacy in patients with allergic rhinitis in the Chinese Han population
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.27278
Abstract: H1‐antihistamine has been shown to be effective in treating patients with allergic rhinitis (AR), but its mechanism is still uncertain. We investigated effects of histamine H1 receptor (HRH1) gene polymorphisms on the efficacy of oral… read more here.
Keywords: allergic rhinitis; chinese han; efficacy; gene ... See more keywords
Structure‐Activity Relationship of Hetarylpropylguanidines Aiming at the Development of Selective Histamine Receptor Ligands†
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DOI: 10.1002/open.201900011
Abstract: Abstract New classes of alkylated hetarylpropylguanidines with different functionality and variation in spacer length were synthesized to determine their behavior at the four histamine receptor (H1R, H2R, H3R, H4R) subtypes. Alkylated guanidines with different terminal… read more here.
Keywords: receptor; structure activity; activity relationship; histamine receptor ... See more keywords
Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103071
Abstract: A novel series of 4-pyridylpiperazine derivatives with varying alkyl linker length and eastern part substituents proved to be potent histamine H3 receptor (hH3R) ligands in the nanomolar concentration range. While paying attention to their alkyl… read more here.
Keywords: affinity; alkyl linker; histamine receptor; methylene ... See more keywords
The dual-active histamine H3 receptor antagonist and acetylcholine esterase inhibitor E100 ameliorates stereotyped repetitive behavior and neuroinflammation in sodium valproate induced autism in mice.
Sign Up to like & getrecommendations! Published in 2019 at "Chemico-biological interactions"
DOI: 10.1016/j.cbi.2019.108775
Abstract: Postnatal exposure to valproic acid (VPA) in rodents induces autism-like neurobehavioral defects which are comparable to the motor and cognitive deficits observed in humans with autism spectrum disorder (ASD). Histamine H3 receptor (H3R) and acetylcholine… read more here.
Keywords: acetylcholine esterase; repetitive behavior; autism; dual active ... See more keywords
Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.09.074
Abstract: The involvement of histamine H4 receptor (H4R) in immune cells chemotaxis and mediator release makes it an attractive target for the treatment of inflammation disorders. A decade of medicinal chemistry efforts has led to several… read more here.
Keywords: virtual screening; discovery; chemistry; histamine receptor ... See more keywords
Novel pyrrolidinone derivative lacks claimed histamine H3 receptor stimulation in receptor binding and functional studies.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112150
Abstract: Since the discovery and early characterization of the histamine H3 receptor (H3R) in the 1980's, predominantly imidazole-based agonists were presented to the scientific community such as Nα-methylhistamine (Nα-MeHA) or (R)-α-methylhistamine ((R)α-MeHA). Whereas therapeutic applications have… read more here.
Keywords: novel pyrrolidinone; lacks claimed; pyrrolidinone derivative; derivative lacks ... See more keywords
Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer's disease.
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DOI: 10.1016/j.ejmech.2020.112743
Abstract: Design and development of multitarget-directed ligands (MTDLs) has become a very important approach in the search of new therapies for Alzheimer's disease (AD). In our present research, a number of xanthone derivatives were first designed… read more here.
Keywords: alzheimer disease; multitarget; design new; inhibitory activity ... See more keywords
Histamine H4 receptor mediates chemotaxis of human lung mast cells
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DOI: 10.1016/j.ejphar.2018.08.028
Abstract: ABSTRACT The diverse effects of histamine are mediated by discrete histamine receptors. The principal repository of histamine in the body is the mast cell. However, the effects of histamine on mast cells, especially those of… read more here.
Keywords: mast cells; human lung; histamine receptor; histamine ... See more keywords
Preliminary study of histamine H4 receptor expressed on human CD4+ T cells and its immunomodulatory potency in the IL-17 pathway of psoriasis.
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DOI: 10.1016/j.jdermsci.2017.05.011
Abstract: BACKGROUND Previous studies have shown the expression of histamine H4 receptor (H4R) on CD4+ T cells, especially human CD4+ Th2-polarized T cells. OBJECTIVE This study aimed to investigate the role of H4R on these effector… read more here.
Keywords: cd4 cells; h4r; expression; psoriasis ... See more keywords
Striatal Signaling Regulated by the H3R Histamine Receptor in a Mouse Model of tic Pathophysiology
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DOI: 10.1016/j.neuroscience.2018.09.035
Abstract: Histamine dysregulation has been identified as a rare genetic cause of tic disorders; mice with a knockout of the histidine decarboxylase (Hdc) gene represent a promising model of this pathophysiology. How alterations in the histamine… read more here.
Keywords: model; h3r histamine; hdc; receptor ... See more keywords