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Histamine H1 receptors

L-H Cheng, J-C Lee, P-C Wu, Y-Y Lin, Y-H Chu, H-W Wang
BACKGROUND: Azelastine hydrochloride (azelastine) nasal spray is a histamine receptor-1 (H1) antagonist often used in treating allergic rhinitis to relieve its symptoms. However, the effects of azelastine to influence decongestion on human nasal mucosa in patients with allergic rhinitis are not yet fully explored and merit further exploration. The effects of azelastine on the vasocontractile responses generated by smooth muscles in the vascular structures of human nasal mucosa were investigated directly in vitro...
March 19, 2019: Rhinology
Fu-Ming Tsai, Chao-Hsu Li, Lu-Kai Wang, Mao-Liang Chen, Ming-Cheng Lee, Yi-Ying Lin, Chun-Hua Wang
Ebastine is a second-generation histamine H1 receptor antagonist that is used to attenuate allergic inflammation. Ebastine has also shown to affect hair loss; however, the immunoregulatory effect of ebastine cannot completely exclude the possibility of spontaneous hair regrowth in ebastine-treated mice. In this study, we examined the effects of ebastine on the growth of human follicle dermal papilla cells (HFDPC) using a WST-1 cell proliferation assay and a bromodeoxyuridine incorporation assay. Ebastine was shown to significantly increase the proliferation of HFDPC...
2019: BioMed Research International
Steffen Pockes, David Wifling, Armin Buschauer, Sigurd Elz
New classes of alkylated hetarylpropylguanidines with different functionality and variation in spacer length were synthesized to determine their behavior at the four histamine receptor (H1 R, H2 R, H3 R, H4 R) subtypes. Alkylated guanidines with different terminal functional groups and varied basicity, like amine, guanidine and urea were developed, based on the lead structure SK&F 91486 ( 2 ). Furthermore, heteroatomic exchange at the guanidine structure of 2 led to simple analogues of the lead compound...
March 2019: ChemistryOpen
Zane Stromberga, Russ Chess-Williams, Christian Moro
The mechanisms underlying bladder contractile disorders such as overactive bladder are not fully understood, and there is limited understanding of the receptor systems modulating spontaneous bladder contractions. We investigated the potential for histamine to have a role in mediating contractility of the urothelium with lamina propria (U&LP) or detrusor via the H1-H4 histamine receptor subtypes. Isolated strips of porcine U&LP or detrusor smooth muscle were mounted in gassed Krebs-bicarbonate solution and responses to histamine obtained in the absence and presence of selective receptor antagonists...
March 7, 2019: Scientific Reports
Agnieszka Matuszewska, Beata Nowak, Diana Jędrzejuk, Marcin Landwójtowicz, Marek Bolanowski, Wojciech Dziewiszek, Anna Merwid-Ląd, Ewa Szeląg, Krzysztof Zduniak, Joanna Kwiatkowska, Adam Szeląg
BACKGROUND: Fenspiride is an antagonist of H1-histamine receptors that is used to treat acute and chronic respiratory tract infections and otitis media in children and adolescents. OBJECTIVES: The aim of the study was to assess the influence of long-term administration of fenspiride on bone mineral density (BMD) and bone turnover in young growing rats. MATERIAL AND METHODS: The experiment was carried out on 18 young (8-week-old) male Wistar rats receiving either fenspiride 15 mg/kg intragastrically (ig) (group F) or saline solution 4 mL/kg ig (group C) for 3 months...
March 6, 2019: Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University
Sarah Ehling, Wolfgang Bäumer, Mark G Papich
BACKGROUND: Histamine type-1 (H1) receptor antagonists such as diphenhydramine are frequently used for treatment of pruritus in dogs, yet therapeutic efficacy for allergic disorders is reported to be highly variable. Dimenhydrinate is a salt of diphenhydramine and 8-chlorotheophylline, and has been reported to produce superior oral absorption of diphenhydramine. HYPOTHESIS/OBJECTIVE: To determine the pharmacokinetic and pharmacodynamic properties of diphenhydramine in dogs after intravenous (1 mg/kg) and oral (5 mg/kg) administration, and when given orally as dimenhydrinate at a dose of 10 mg/kg (≈5 mg/kg diphenhydramine)...
February 19, 2019: Veterinary Dermatology
John Wesson Ashford
In this issue, an article by La et al. provides evidence that trazodone delayed cognitive decline in 25 participants with Alzheimer's disease (AD), mild cognitive impairment, or normal cognition. For participants considered to have AD pathology, trazodone non-users declined at a rate 2.4 times greater than those taking trazodone for sleep over a 4-year period. In the analysis of sleep complaints, the relationship between trazodone, a widely used medication for sleep problems in the elderly, and cognition was associated with subjective improvement of sleep disruption...
2019: Journal of Alzheimer's Disease: JAD
Francesco De Logu, Lorenzo Landini, Malvin N Janal, Simone Li Puma, Francesco De Cesaris, Pierangelo Geppetti, Romina Nassini
BACKGROUND: Administration of endogenous mediators or exogenous chemicals in migraine patients provoke early headaches and delayed migraine-like attacks. Although migraine provoking substances are normally vasodilators, dilation of arterial vessels does not seem to be the sole contributing factor, and the underlying mechanisms of the delayed migraine pain are mostly unknown. Sustained mechanical allodynia is a common response associated with the local administration of various proalgesic substances in experimental animals and humans...
February 14, 2019: Journal of Headache and Pain
Rujia Liao, Youchao Chen, Li Cheng, Lishi Fan, Han Chen, Yushan Wan, Yi You, Yanrong Zheng, Lei Jiang, Zhong Chen, Xiangnan Zhang, Weiwei Hu
The neurological recovery following traumatic brain injury (TBI) is limited, largely due to a deficiency in neurogenesis. The present study explores the effects of histamine H3 receptor (H3R) antagonism on TBI and mechanisms related to neurogenesis. H3R antagonism or H3R gene knockout alleviated neurological injury in the late phase of TBI, and also promoted neuroblast differentiation to enhance neurogenesis through activation of the histaminergic system. Histamine H1 receptor, but not H2 receptor, in neural stem cells is shown to be essential for this promotion by using Hrh1fl/fl ;NestinCreERT2 and Hrh2fl/fl ;NestinCreERT2 mice...
January 22, 2019: Stem Cell Reports
G G Bruer, P Hagedorn, M Kietzmann, A F Tohamy, V Filor, E Schultz, S Mielke-Kuschow, J Meissner
BACKGROUND: H1 receptor antagonists are commonly used for the treatment of allergic diseases. The aim of this study was to find out, if antihistaminic compounds like mepyramine have the ability to influence the activity of antibacterials. Therefore, the checkerboard method was chosen to detect these possible effects in vitro. Studies were performed with two different Escherichia coli (E. coli) strains as test microbes, treated with antibacterials in combination with mepyramine. RESULTS: The minimum inhibitory concentration (MIC) of E...
February 11, 2019: BMC Veterinary Research
Natalia Kordulewska, Anna Cieślińska, Ewa Fiedorowicz, Beata Jarmołowska, Elżbieta Kostyra
PURPOSE: Fexofenadine (FXF) is the active metabolite of terfenadine with selective peripheral H1 receptor antagonist activity. FXF is a third-generation antihistamine, non-sedating, rapid and very long acting used in symptoms associated with allergic diseases such as allergic rhinitis, asthma and dermatitis. The pleiotropic effects of histamine are mediated by four types of receptors that belong to the G-protein-coupled receptor family: histamine H1 receptor (HRH-1), histamine H2 receptor, histamine H3 receptor, and histamine H4 receptor...
2019: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
Cristina Grange, Maura Gurrieri, Roberta Verta, Roberto Fantozzi, Alessandro Pini, Arianna Carolina Rosa
Starting from the histamine role in the renal haemodynamic, over time, spare evidence suggested a wider range of action on renal function and renewed the interest on the pathophysiological role of histamine in the kidney. This review intends to provide an up-to-date focus on this topic. According to the intrarenal production of histamine and the renal presence of its receptors, the histaminergic machinery appears to be well suited. The distribution of histamine receptors supports their differential effects but do not exclude the redundancy of H1 and H2 receptors in renal haemodynamics, the complementary role of H1 and H4 receptors in renal filtration and reabsorption, and the dichotomy between local and neuronal H1 and H3 receptors...
February 11, 2019: British Journal of Pharmacology
Sebastian C Holst, Esther Werth, Hans-Peter Landolt
Pharmacotherapy of Sleep-Wake Disorders Abstract. Sleep is a complex behavior, coordinated by many different brain regions and neurotransmitters. These neurochemical systems can be pharmacologically influenced to modulate wakefulness and sleep. Excessive daytime sleepiness (EDS) is often treated with dopaminergic drugs, which in mild cases range from caffeine via (ar)modafinil to amphetamine derivatives. Tricyclic antidepressants and melatonin-based drugs are also used to promote alertness, but to a lesser extent...
January 2019: Praxis
Joanna Sniecikowska, Monika Głuch-Lutwin, Adam Bucki, Anna Więckowska, Agata Siwek, Magdalena Jastrzębska-Więsek, Anna Partyka, Daria Wilczyńska, Karolina Pytka, Krzysztof Pociecha, Agnieszka Cios, Elżbieta Wyska, Anna Wesołowska, Maciej H Pawłowski, Mark Varney, Adrian Newman-Tancredi, Marcin Kołaczkowski
Novel 1-(1-benzoylpiperidin-4-yl)methanamine derivatives were designed as 'biased agonists' of serotonin 5-HT1A receptors. Compounds were tested in signal transduction assays (ERK1/2 phosphorylation, cAMP inhibition, Ca2+ mobilization and β-arrestin recruitment) which identified ERK1/2 phosphorylation-preferring aryloxyethyl derivatives. The novel series showed high 5 HT1A receptor affinity, >1000-fold selectivity versus noradrenergic α1, dopamine D2, 5-HT2A, histamine H1 and muscarinic M1 receptors, and favorable drug-likeness properties (CNS-MPO, Fsp3, LELP)...
February 5, 2019: Journal of Medicinal Chemistry
Keisuke Obara, Lin Ao, Tsukasa Ogawa, Takumi Ikarashi, Fumiko Yamaki, Kazuhiro Matsuo, Takashi Yoshio, Yoshio Tanaka
The present study aimed to investigate the potential inhibitory effects of 21 clinically available hypnotics on acetylcholine (ACh)-induced contractions in rat urinary bladder smooth muscle (UBSM) in order to predict whether these hypnotics could induce voiding impairment. ACh-induced contraction in rat UBSM was inhibited only by diphenhydramine (a histamine H1 receptor antagonist) at a concentration that was clinically relevant. ACh-induced contraction was also significantly inhibited by flurazepam (a benzodiazepine hypnotic) and suvorexant (an orexin receptor antagonist), albeit at concentrations that substantially exceeded clinically achievable blood levels...
2019: Biological & Pharmaceutical Bulletin
Matthew R Ely, Dylan C Sieck, Joshua E Mangum, Emily A Larson, Leandro C Brito, Christopher T Minson, John R Halliwill
Histamine is released within skeletal muscle during exercise. In humans, antihistamines have no effect on speed, power output, or time-to-completion of short-duration high-intensity exercise. In mice, blocking histamine's actions decreases speed and duration of endurance tasks. It is unknown if these opposing outcomes are the result of differences in histamine's actions between species or are related to duration and/or intensity of exercise, as blocking histamine during endurance exercise has not been examined in humans...
January 25, 2019: Medicine and Science in Sports and Exercise
Antonela Díaz Nebreda, Carlos Daniel Zappia, Angela Rodríguez González, Ana Sahores, Máximo Sosa, Valeria Burghi, Federico Monczor, Carlos Davio, Natalia Fernández, Carina Shayo
Histamine [2-(4-Imidazolyl)-ethylamine] modulates different biological processes, through histamine H1 and H2 receptors, and their respective blockers are widely used in treating allergic and gastric acid-related disorders. Histamine H1 and H2 receptor crossdesensitization and cointernalization induced by its agonists have been previously described. In this study, we show how this crosstalk determines the response to histamine H1 and H2 receptor inverse agonists and how histamine H1 and H2 receptor inverse agonists interfere with the other receptor's response to agonists...
January 24, 2019: European Journal of Pharmacology
Uwe Matterne, Merle Margarete Böhmer, Elke Weisshaar, Aldrin Jupiter, Ben Carter, Christian J Apfelbacher
BACKGROUND: The symptoms of eczema can lead to sleeplessness and fatigue and may have a substantial impact on quality of life. Use of oral H1 antihistamines (H1 AH) as adjuvant therapy alongside topical agents is based on the idea that combining the anti-inflammatory effects of topical treatments with the blocking action of histamine on its receptors in the skin by H1 AH (to reduce the principal symptom of itch) might magnify or intensify the effect of treatment. Also, it would be unethical to compare oral H1 AH alone versus no treatment, as topical treatment is the standard management for this condition...
January 22, 2019: Cochrane Database of Systematic Reviews
Sikai Li, Tsugunobu Andoh, Qun Zhang, Daisuke Uta, Yasushi Kuraishi
Chronic renal failure (CRF) is a progressive disease with severe pruritus and dry skin as the major symptoms. However, the mechanisms of CRF-induced pruritus remain unclear. In this study, 5/6 nephrectomized (NPCT) mice were used as a mouse model of CRF. Serum concentrations of blood urea nitrogen and creatinine in 5/6 NPCT mice were increased. The stratum corneum water content in the skin of 5/6 NPCT mice was decreased. These findings suggest that 5/6 nephrectomy in mice results in a phenotype resembling human CRF...
January 16, 2019: European Journal of Pharmacology
Noriyasu Hirasawa
Histamine is a well-known mediator of inflammation that is released from mast cells and basophils. To date, many studies using histamine receptor antagonists have shown that histamine acts through four types of receptors: H1, H2, H3, and H4. Thus, histamine plays more roles in various diseases than had been predicted. However, our knowledge about histamine-producing cells and the molecular mechanisms underlying histamine production at inflammatory sites is still incomplete. The histamine producing enzyme, histidine decarboxylase (HDC), is commonly induced at inflammatory sites during the late and chronic phases of both allergic and non-allergic inflammation...
January 16, 2019: International Journal of Molecular Sciences
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