keyword
MENU ▼
Read by QxMD icon Read
search

Histamine receptors

keyword
https://www.readbyqxmd.com/read/29792195/histamine-activates-inflammatory-response-and-depresses-casein-synthesis-in-mammary-gland-of-dairy-cows-during-sara
#1
Guangjun Chang, Lailai Wang, Nana Ma, Wenwen Zhang, Huanmin Zhang, Hongyu Dai, Xiangzhen Shen
BACKGROUND: Mounting evidences observed that subacute ruminal acidosis (SARA) induced by high concentration (HC) diet increases the translocation of histamine from digestive tract into circulation causing a diverse of diseases in dairy cows. However, it is largely unknown how it does affect the function of mammary gland and milk quality. Hence, this study aims to observe the effects of histamine derived from the digestive tract on the inflammatory response and casein synthesis in the mammary glands during SARA...
May 23, 2018: BMC Veterinary Research
https://www.readbyqxmd.com/read/29791754/atp-triggers-a-robust-intracellular-ca-2-mediated-signalling-pathway-in-human-synovial-fibroblasts
#2
Kondo C, R B Clark, T Y Kim, Belke D, Banderali U, R T Szerencsei, A H Jalloul, P P M Schnetkamp, Spitzer Kw, Giles Wr
NEW FINDINGS: What is the central question of this study? In human articular joints, the synovial fibroblast HSF cell population has essential functions including secretion of lubricants. We address some remaining questions concerning activation-secretion coupling by characterizing the main [Ca2+ ]i signalling pathways activated by ATP. What is the main finding and its importance? In HSF ATP acts through a linked G-protein (Gq ) and phospholipase C signalling mechanisms to produce IP-3 which markedly enhances release of Ca2+ from the endoplasmic reticulum...
May 23, 2018: Experimental Physiology
https://www.readbyqxmd.com/read/29784282/characterization-of-human-decidual-mast-cells-and-establishment-of-a-culture-system
#3
Takayuki Matsuno, Shota Toyoshima, Tomomi Sakamoto-Sasaki, Jun-Ichi Kashiwakura, Akira Matsuda, Yasuo Watanabe, Hiromitsu Azuma, Kei Kawana, Tatsuo Yamamoto, Yoshimichi Okayama
BACKGROUND: Although rodent decidual mast cells (MCs) reportedly play an important role in implantation and placenta formation, the characterization of human decidual MCs has been not well clarified. The aims of this study were to investigate the distribution and characteristics of MCs in human decidua and to establish a culture system for decidua-derived MCs. METHODS: Decidual tissues were obtained from patients who underwent a legal elective abortion (6th week to 9th week of pregnancy), and decidual MCs were enzymatically dispersed...
May 18, 2018: Allergology International: Official Journal of the Japanese Society of Allergology
https://www.readbyqxmd.com/read/29768271/direct-potentiation-of-capsaicin-current-by-histamine-and-its-effect-by-suplatast-on-rat-trigeminal-ganglia-neurons
#4
Jian-Rong Zhou, Tetsuya Shirasaki, Fumio Soeda, Kazumi Yokomizo, Kazuo Takahama
In this study, we investigated the effect of histamine on capsaicin-induced current and its influence by suplatast in rat trigeminal ganglia neurons using a patch-clamp technique. We found that histamine directly potentiated capsaicin-induced currents in rat sensory neurons, and suplatast had little effect on this potentiation. Since it has been known that suplatast suppresses histamine release from mast cells, it is possible that suplatast inhibits the activation of nociceptive fibers in the pathological condition via prevention of histamine-induced potentiation of the transient receptor potential vanilloid 1 receptor-mediated currents...
May 16, 2018: Pharmacology
https://www.readbyqxmd.com/read/29765253/use-of-histamine-h-2-receptor-antagonists-and-outcomes-in-patients-with-heart-failure-a-nationwide-population-based-cohort-study
#5
Kasper Adelborg, Jens Sundbøll, Morten Schmidt, Hans Erik Bøtker, Noel S Weiss, Lars Pedersen, Henrik Toft Sørensen
Background: Histamine H2 receptor activation promotes cardiac fibrosis and apoptosis in mice. However, the potential effectiveness of histamine H2 receptor antagonists (H2RAs) in humans with heart failure is largely unknown. We examined the association between H2RA initiation and all-cause mortality among patients with heart failure. Methods: Using Danish medical registries, we conducted a nationwide population-based active-comparator cohort study of new users of H2RAs and proton pump inhibitors (PPIs) after first-time hospitalization for heart failure during the period 1995-2014...
2018: Clinical Epidemiology
https://www.readbyqxmd.com/read/29763312/deep-sea-derived-butyrolactone-i-suppresses-ovalbumin-induced-anaphylaxis-by-regulating-mast-cell-function-in-a-murine-model
#6
Qingmei Liu, Chun-Lan Xie, Yuanyuan Gao, Bo Liu, Weixiang Lin, Hong Liu, Min-Jie Cao, Wen-Jin Su, Xianwen Yang, Guang-Ming Liu
Deep-sea-derived butyrolactone I (BTL-I) which was identified as a type of butanolide was isolated from Aspergillus sp. Ovalbumin (OVA)-induced BALB/c anaphylaxis was established to explore the anti-food allergic activity of BTL-I. As results, BTL-I was able to alleviate OVA-induced allergy symptoms, reduce the levels of histamine and mouse mast cell proteinases, inhibit OVA-specific IgE, and decrease the population of mast cells in the spleen and mesenteric lymph nodes. BTL-I also significantly suppressed mast-dependent passive cutaneous anaphylaxis...
May 15, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29749407/peripheral-n-methyl-d-aspartate-receptor-localization-and-role-in-gastric-acid-secretion-regulation-immunofluorescence-and-pharmacological-studies
#7
Iuliia Golovynska, Tatiana V Beregova, Tatiana M Falalyeyeva, Ludmila I Stepanova, Sergii Golovynskyi, Junle Qu, Tymish Y Ohulchanskyy
The enteric nervous system (ENS) and a glutamate receptor (GluR), N-methyl-D-aspartate receptor (NMDAR), participate in gastric acid secretion (GAS) regulation. NMDARs are localized in different stomach cells; however, knowledge of NMDAR expression and function in the ENS is limited. In the present study, we clarified the types of stomach cells that express the NMDARs that are involved in GAS regulation. The pharmacological method of isolated stomach perfusion by Ghosh and Shild combined with direct mapping of NMDARs by fluorescence microscopy in the rat stomach was employed...
May 10, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29742501/modulation-of-mast-cell-toll-like-receptor-3-expression-and-cytokines-release-by-histamine
#8
Guogang Xie, Feng Wang, Xia Peng, Yuting Liang, Haiwei Yang, Li Li
BACKGROUND/AIMS: As a major inflammatory molecule released from mast cell activation, histamine has been reported to regulate TLRs expression and cytokine production in inflammatory cells present in the microenvironment. In this study, we determined the ability of histamine to modulate TLRs expression and cytokine production in mast cells. METHODS: HMC-1 and P815 cells were exposed to various concentrations of histamine in the presence or absence of histamine antagonist for 2, 6 or 16 h...
May 4, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29741272/proton-pump-inhibitor-and-histamine-2-receptor-antagonist-use-and-risk-of-liver-cancer-in-two-population-based-studies
#9
K T Tran, Ú C McMenamin, B Hicks, P Murchie, A P Thrift, H G Coleman, L Iversen, B T Johnston, A J Lee, C R Cardwell
BACKGROUND: Proton pump inhibitors (PPIs) and histamine-2 receptor antagonists (H2RAs) are commonly used. PPIs have been shown to promote liver cancer in rats; however, only one study has examined the association in humans. AIMS: To investigate PPIs and H2RAs and risk of primary liver cancer in two large independent study populations. METHODS: We conducted a nested case-control study within the Primary Care Clinical Informatics Unit (PCCIU) database in which up to five controls were matched to cases with primary liver cancer, recorded by General Practitioners...
May 9, 2018: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29738736/organic-cation-transporter-3-a-cellular-mechanism-underlying-rapid-non-genomic-glucocorticoid-regulation-of-monoaminergic-neurotransmission-physiology-and-behavior
#10
REVIEW
Paul J Gasser, Christopher A Lowry
Corticosteroid hormones act at intracellular glucocorticoid receptors (GR) and mineralocorticoid receptors (MR) to alter gene expression, leading to diverse physiological and behavioral responses. In addition to these classical genomic effects, corticosteroid hormones also exert rapid actions on physiology and behavior through a variety of non-genomic mechanisms, some of which involve GR or MR, and others of which are independent of these receptors. One such GR-independent mechanism involves corticosteroid-induced inhibition of monoamine transport mediated by "uptake2 " transporters, including organic cation transporter 3 (OCT3), a low-affinity, high-capacity transporter for norepinephrine, epinephrine, dopamine, serotonin and histamine...
May 5, 2018: Hormones and Behavior
https://www.readbyqxmd.com/read/29735707/flight-motor-networks-modulate-primary-olfactory-processing-in-the-moth-manduca-sexta
#11
Phillip D Chapman, Rex Burkland, Samual P Bradley, Benjamin Houot, Victoria Bullman, Andrew M Dacks, Kevin C Daly
Nervous systems must distinguish sensory signals derived from an animal's own movements (reafference) from environmentally derived sources (exafference). To accomplish this, motor networks producing reafference transmit motor information, via a corollary discharge circuit (CDC), to affected sensory networks, modulating sensory function during behavior. While CDCs have been described in most sensory modalities, none have been observed projecting to an olfactory pathway. In moths, two mesothoracic to deutocerebral histaminergic neurons (MDHns) project from flight sensorimotor centers in the mesothoracic neuromere to the antennal lobe (AL), where they provide the sole source of histamine (HA), but whether they represent a CDC is unknown...
May 7, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29731751/unique-action-of-interleukin-18-on-t-cells-and-other-immune-cells
#12
REVIEW
Kenji Nakanishi
Interleukin (IL)-18 was originally discovered as a factor that enhances interferon (IFN)-γ production by anti-CD3-stimulated Th1 cells, particularly in association with IL-12. IL-12 is a cytokine that induces development of Th1 cells. IL-18 cannot induce Th1 cell development, but has the capacity to activate established Th1 cells to produce IFN-γ in the presence of IL-12. Thus, IL-18 is regarded as a proinflammatory cytokine that facilitates type 1 responses. However, in the absence of IL-12 but presence of IL-2, IL-18 stimulates natural killer cells, NKT cells, and even established Th1 cells to produce IL-3, IL-9, and IL-13...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29729290/anticonvulsant-evaluation-of-novel-non-imidazole-histamine-h-3-r-antagonists-in-different-convulsion-models-in-rats
#13
Alaa Alachkar, Gniewomir Latacz, Agata Siwek, Annamaria Lubelska, Ewelina Honkisz, Anna Gryboś, Dorota Łażewska, Jadwiga Handzlik, Holger Stark, Katarzyna Kiec-Kononowicz, Bassem Sadek
Novel non-imidazole histamine H3 receptor (H3R) antagonists (2-8) were developed and assessed for in-vitro antagonist binding affinities at the human histamine H1-H4R. These novel H3R antagonists (2-8) were examined in-vivo for anticonvulsant effects in three different convulsion models in male adult rats. Compound 6 significantly and dose-dependently exhibited decreased duration of tonic hind limb extension (THLE) in the maximal electroshock (MES)- and fully protected animals against pentylenetetrazole (PTZ)-induced convulsion, following acute systemic administration (5, 10, and 20 mg/kg, i...
May 2, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29728446/tas05567-a-novel-potent-and-selective-spleen-tyrosine-kinase-inhibitor-abrogates-immunoglobulin-mediated-autoimmune-and-allergic-reactions-in-rodent-models
#14
Hiroaki Hayashi, Ryusuke Kaneko, Shunsuke Demizu, Daichi Akasaka, Manabu Tayama, Takafumi Harada, Hiroki Irie, Yoshio Ogino, Naoko Fujino, Eiji Sasaki
Spleen tyrosine kinase (Syk) is involved in regulation of B-cell receptor (BCR) and Fc receptor (FcR) downstream signal pathways. Syk plays an essential role in production of inflammatory mediators and differentiation in various immune cells and is therefore an attractive target for treating inflammatory conditions, such as autoimmune and allergic diseases. We identified TAS05567 as a highly selective Syk inhibitor and evaluated its therapeutic potential in animal models. In vitro biochemical assays were performed with available kinase assay panels...
May 4, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29728020/-molecular-mechanism-of-bupleuri-radix-and-scutellariae-radix-drug-pair-for-depression-based-on-integrative-pharmacology-platform-of-traditional-chinese-medicine
#15
Jian-Ting Wang, Shang Wang, Song-Lin Liu, Yan-Chun Wang, Jia-Geng Li, Yu Chen
Xiaochaihu decoction is a classic prescription of traditional Chinese medicine. Modern research has proved its anti-depression effect. However, its pharmacological mechanism for anti-depression effect is difficult to be unveiled because of the complexity of compound Chinese medicines. Bupleuri Radix and Scutellariae Radix is the core drug pair of Xiaochaihu decoction. In this research, Bupleuri Radix and Scutellariae Radix were analyzed by the integrative pharmacology platform to study its molecular mechanism for anti-depression...
April 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29723785/synthesis-and-biological-activity-of-novel-tert-butyl-and-tert-pentylphenoxyalkyl-piperazine-derivatives-as-histamine-h-3-r-ligands
#16
Katarzyna Szczepańska, Tadeusz Karcz, Szczepan Mogilski, Agata Siwek, Kamil J Kuder, Gniewomir Latacz, Monika Kubacka, Stefanie Hagenow, Annamaria Lubelska, Agnieszka Olejarz, Magdalena Kotańska, Bassem Sadek, Holger Stark, Katarzyna Kieć-Kononowicz
As a continuation of our search for novel histamine H3 receptor ligands, a series of twenty four new tert-butyl and tert-pentyl phenoxyalkylamine derivatives (2-25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer were evaluated for their binding properties at human histamine H3 receptor (hH3 R). The highest affinities were observed for 4-pyridyl derivatives 4, 10, 16 and 22 (Ki  = 16.0-120 nM). As it has been shown in docking studies, those specific heteroaromatic 4-N piperazine substituents might interact with one of the key receptor interacting amino acids...
April 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29722587/the-preclinical-discovery-and-development-of-cariprazine-for-the-treatment-of-schizophrenia
#17
Anna Wesołowska, Anna Partyka, Magdalena Jastrzębska-Więsek, Marcin Kołaczkowski
Cariprazine is approved in the United States and Europe for the treatment of manic or mixed episodes associated with bipolar I disorder and for the treatment of schizophrenia in adult patients. It is typically administered orally once a day (a dose range 1.5 - 6 mg/day), does require titration, and may be given with or without food. It has a half-life of 2 - 4 days with an active metabolite that has a terminal half-life of 2 - 3 weeks. Areas covered: This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits...
May 3, 2018: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29704723/identification-of-novel-%C3%AE-lactams-and-pyrrolidinone-derivatives-as-selective-histamine-3-receptor-h3r-modulators-as-possible-anti-obesity-agents
#18
Anirban Ghoshal, Ajeet Kumar, Doddapaneni Yugandhar, Chandan Sona, Sunu Kuriakose, Kommu Nagesh, Mamunur Rashid, Sandeep K Singh, Muhammad Wahajuddin, Prem N Yadav, Ajay K Srivastava
Four series of structurally related β-lactams, 2,5-pyrrolidinediones, azaspirodecatrienediones (ASDT) and dihydropyrroloquinoxalinetriones (DPQT) were synthesized by utilizing post-Ugi modifications in one-pot, and their activity towards human histamine-3 receptor (H3R) was evaluated. Out of 94 compounds, screened against histamine-3 receptor (H3R), 21 compounds showed high H3R selective agonist property with EC50 values ranging from 187 nM to 0.1 nM, whereas none of the compound was found to have the affinity towards other receptors of histamine family such as histamine H1, H2, and H4 receptor...
April 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29702735/effects-of-ugt1a1-cyp3a5-and-abcb1-genetic-variants-on-pharmacokinetics-of-antihistamine-drug-mizolastine-in-chinese-healthy-volunteers
#19
Pu Li, Min-Ji Wei, Zhi-Yuan Zhang, Sheng-Ju Yin, Xin Wang, Ya-Qing Lou, Zi-Sheng Kang, Yuan Lu, Xuan Wei, Suo-Di Zhai, Guo-Liang Zhang
Mizolastine is a selective histamine H1 receptor antagonist for chronic urticaria or allergic rhinitis. We investigated whether the variant genotypes of metabolic enzymes UGT1A1, CYP3A5 and transporter ABCB1 influence pharmacokinetic phenotype of substrate mizolastine in Chinese volunteers. Genotyping of single nucleotide polymorphisms (SNPs) in UGT1A1*6 (G211A), CYP3A5*3 (A6986G) and ABCB1 (C3435T) were determined by the pyrosequencing method. After a single oral dose of 10 mg mizolastine, the plasma concentrations were measured using validated high performance liquid chromatography (HPLC) in 24 Chinese healthy volunteers...
April 27, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29701013/visualization-of-the-activation-of-the-histamine-h3-receptor-h3r-using-novel-fluorescence-resonance-energy-transfer-biosensors-and-their-potential-application-to-the-study-of-h3r-pharmacology
#20
Ying Liu, Hong Zeng, John D Pediani, Richard J Ward, Lu-Yao Chen, Nan Wu, Li Ma, Mei Tang, Yang Yang, Su An, Xiao-Xi Guo, Qian Hao, Tian-Rui Xu
Activation of the Histamine-3 receptor (H3R) is involved in memory processes and cognitive action, whilst blocking H3R activation can slow the progression of neurological disorders such as Alzheimer's disease, schizophrenia and narcolepsy. To date however no direct way to examine the activation of H3R has been utilised. Here, we describe a novel biosensor which can visualise the activation of H3R through an intramolecular Fluorescence Resonance Energy Transfer (FRET) signal. To achieve this, we constructed an intramolecular H3R FRET sensor with cyan fluorescent protein (CFP) attached at the C-terminus and yellow fluorescent protein (YFP) inserted into the third intracellular loop...
April 26, 2018: FEBS Journal
keyword
keyword
80879
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"