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- | Journal: Rapidly and accurately screening histidine decarboxylase inhibitors from Radix Paeoniae alba using ultrafiltration-high performance liquid chromatography/mass spectrometry combined with enzyme channel blocking and directional enrichment technique. (Pubmed Central) - Mar 13, 2023
Furthermore, gallic acid (IC 1.8
- | Journal: Antagonism of histamine H receptor promotes angiogenesis following focal cerebral ischemia. (Pubmed Central) - Nov 3, 2022
In conclusion, this study demonstrates that HR antagonism promotes angiogenesis after cerebral ischemia, which is independent of activation of histaminergic neurons, but related to the HR on vascular endothelial cells and its interaction with Annexin A2. Thus, HR antagonists might be promising drug candidates to improve angiogenesis and neurological recovery after ischemic stroke.
- | carboplatin / Generic mfg.
Journal: Histidine decarboxylase inhibitors: a novel therapeutic option for the treatment of leydigioma. (Pubmed Central) - Oct 6, 2022
We, therefore, evaluated for the first time the antitumor efficacy of two histidine decarboxylase inhibitors (α-methyl-dl-histidine dihydrochloride (α-MHD) and epigallocatechin gallate (EGCG)), alone and combined with carboplatin, in two preclinical models of LCT...Testicular and body weights remained unaltered. On the basis of this study, histidine decarboxylase may emerge as a novel pharmacological target for LCT treatment.
- | cetirizine oral / Generic mfg.
Preclinical, Journal: Ameliorative Effect of a Neoteric Regimen of Catechin plus Cetirizine on Ovalbumin-Induced Allergic Rhinitis in Rats. (Pubmed Central) - Jun 25, 2022
Catechin binds the catalytic residue S354, unlike cetirizine. The anti-allergic effects of catechin can be explained by HDC inhibition and possible antihistaminic activity.
- | Preclinical, Journal: Oral histidine intake improves working memory through the activation of histaminergic nervous system in mice. (Pubmed Central) - May 12, 2022
This beneficial effect of histidine on memory was cancelled by intracerebroventricular injection of the HDC inhibitor α-fluoromethylhistidine. These results demonstrate that oral histidine intake replenishes brain histamine and leads to the recovery of impaired working memory induced by sleep deprivation through histaminergic activation.
- | pegylated liposomal doxorubicin / Generic mfg.
Biomarker, Journal: Biomarkers of PEGylated Liposomal Doxorubicin-Induced Hypersensitivity Reaction in Breast Cancer Patients Based on Metabolomics. (Pubmed Central) - May 10, 2022
Moreover, an antihistamine drug, histidine decarboxylase inhibitor, or dietary histidine management could be used as potential preventive measures. Furthermore, metabolomics research could serve as a powerful method to explore biomarkers or uncover mechanisms of drug side effects.
- | Journal: Anti-Allergic Effects of Myrciaria dubia (Camu-Camu) Fruit Extract by Inhibiting Histamine H1 and H4 Receptors and Histidine Decarboxylase in RBL-2H3 Cells. (Pubmed Central) - Jan 26, 2022
These findings indicate that camu-camu fruit extract can be developed to act as a mast cell stabilizer and an anti-histamine. This work also "opens the door" to new investigations using natural products to achieve breakthroughs in allergic disorder treatment.
- | Journal: Anti-Allergic Potential of Cinnamaldehyde via the Inhibitory Effect of Histidine Decarboxylase (HDC) Producing Klebsiella pneumonia. (Pubmed Central) - Apr 10, 2021
A gene expression and Western blotting study revealed that CA significantly downregulated the expressions of MAPKp38/ERK and its downstream pro-allergic mediators that are involved in the signaling pathway in mast cell cytokine synthesis. This study further confirms that CA has the potential to attenuate mast cell activation by inhibiting HDC and modifying the process of allergic disorders.
- | Nitredon (nitrazepam) / Remedica
Journal: Effects of Histamine and Related Compounds on the Central Nervous System (Pubmed Central) - Feb 16, 2021
On the other hand, no significant effects were observed with second generation H-antagonists. These findings suggest that histamine plays an important role in learning and memory via H-receptors, an inhibition of amygdaloid kindled seizures induced by histamine occurred through not only H-receptors but also H-receptors, and that classic H-antagonists can be useful as a effective hypnotic for difficulty in falling asleep.
- | Journal: The novel sophoridine derivate IMB-HDC induced lessened phosphorylation of STAT5a at 694 and 780 and promoted DNA breakage and cell apoptosis via blocking STAT5a nuclear translocation. (Pubmed Central) - Feb 10, 2021
Meanwhile, IMB-HDC that induced the diminished expression of STAT5a target gene contributes to proliferation and leads to apoptosis. More importantly, we give the first evidence that promoting the effect of Tyr694 phosphorylation on nuclear location and subsequent STAT5a target gene transcription depends on Ser780 increased or unchanged phosphorylation and was not correlated with Ser726 phosphorylation.
- carbidopa / Generic mfg.
[VIRTUAL] Histaminergic basis of fatigue in Multiple Sclerosis () - Sep 3, 2020 - Abstract #MSDC2020MSDC_1585;
Conversion systemically from l-histidine to histamine was blocked using histidine decarboxylase inhibitor, lodosyn, which has no access to the brain across the blood brain barrier.All subjects received a fixed dose lodosyn, 50 mg po bid...This novel approach opens up a new avenue to identify drugs that raise brain histamine as a mechanism of treatment of fatigue in MS and possibly other disorders with fatigue where histamine may play a pivotal role in the pathogenesis of this common and severely disabling symptom. Additionally this treatment could also provide an approach to help cognitive impairment in multiple sclerosis since raising brain histamine can facilitate also the enhanced release of a number of neurotransmitters including acetylcholine, implicated in the pathogenesis of cognitive impairment in various disorders including multiple sclerosis.
- | Journal: The lipidated connexin mimetic peptide, SRPTEKT-Hdc, is a potent inhibitor of Cx43 channels with specificity for the pS368 phospho-isoform. (Pubmed Central) - Apr 10, 2020
In contrast, Ca-wave propagation, dye coupling, and dye uptake were largely unaffected (IC: 12.3 μM) by SRPTEKT-Hdc in MDCK43-S368A and -S365D cells, mutations that mimic or favor dephosphorylation at S368. Together, these data indicate that SRPTEKT-Hdc is a potent inhibitor of physiologic Ca-wave signaling mediated specifically by the pS368 phospho-form of Cx43.
- CROSSTALK SIGNALING BETWEEN MAST CELLS, HISTAMINE AND STIMULATOR OF INTERFERON GENE (STING/TMEM173) PROMOTES CHOLANGIOCARCINOMA (CCA) TUMORIGENESIS () - Jan 28, 2020 - Abstract #DDW2020DDW_2832;
MC-derived HA/HR signaling regulates STING expression (dysregulated in CCA) during tumorigenesis. Blocking HDC/HA/HR signaling or targeting STING may be a therapeutic option for patients with intrahepatic CCA
- | Decadron (dexamethasone) / Merck (MSD), Sebifin (terbinafine HCL) / Generic mfg.
Preclinical, Journal: Itching in a trichophytin contact dermatitis mouse model and the antipruritic effect of antifungal agents. (Pubmed Central) - Jan 9, 2020
Blocking HDC/HA/HR signaling or targeting STING may be a therapeutic option for patients with intrahepatic CCA Antifungals can inhibit itching induced by fungal infection through different mechanisms.
- | Journal: Repurposing a Histamine Detection Platform for High-Throughput Screening of Histidine Decarboxylase. (Pubmed Central) - Sep 20, 2019
A pilot HTS screen gave a Z' score > 0.5 and a hit rate of 1.1%, and led to the identification of a validated hit series. Overall, the presented assay should facilitate the discovery of therapeutic HDC inhibitors by acting as a novel tool suitable for large-scale HTS and subsequent interrogation of compound structure-activity relationships.
- | Journal: Lipidated connexin mimetic peptides potently inhibit gap junction-mediated Ca-wave propagation. (Pubmed Central) - Jul 4, 2019
Selective inhibition of intercellular Ca signaling, likely indicative of channel conformation-specific SRPTEKT-Hdc binding, could contribute significantly to the protective effects of these mimetic peptides in settings of injury. Our data also demonstrate that lipidation represents a paradigm for development of highly potent, efficacious and selective mimetic peptide inhibitors of hemichannel and gap junction channel-mediated signaling.
- | Journal: The ellagitannin trimer rugosin G inhibits recombinant human histidine decarboxylase. (Pubmed Central) - Apr 18, 2019
Rugosin G showed potent inhibition compared to ellagitannin monomers and a dimer with macrocyclic structure (oenothein B), suggesting the potent inhibition of rugosin G was attributed to its linear oligomeric conformation. Abbreviations: HDC, histidine decarboxylase; Me2CO, acetone; EtOAc, ethyl acetate.
- | Journal: Inhibiting Histamine Signaling Ameliorates Vertigo Induced by Sleep Deprivation. (Pubmed Central) - Apr 16, 2019
Upregulated HDC in the vestibular and increased CSF concentration of histamine can be detected in the SD mice, indicating vestibular dysfunction which can be ameliorated by both BHOA and DPHM. Histamine signaling inhibition may ameliorate SD-induced vertigo, and histamine can be considered as a potential treatment target.