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α2 receptor

Ken Matsui, Makoto Ozawa, Maki Kiso, Makoto Yamashita, Toshihiko Maekawa, Minoru Kubota, Sumio Sugano, Yoshihiro Kawaoka
Influenza A viruses cause seasonal epidemics and occasional pandemics. The emergence of viruses resistant to neuraminidase (NA) inhibitors and M2 ion channel inhibitors underlines the need for alternate anti-influenza drugs with novel mechanisms of action. Here, we report the discovery of a host factor as a potential target of anti-influenza drugs. By using cell-based virus replication screening of a chemical library and several additional assays, we identified clonidine as a new anti-influenza agent in vitro...
March 15, 2018: Scientific Reports
Guang-Zhe Huang, Mutsuo Taniguchi, Ye-Bo Zhou, Jing-Ji Zhang, Fumino Okutani, Yoshihiro Murata, Masahiro Yamaguchi, Hideto Kaba
The formation of mate recognition memory in mice is associated with neural changes at the reciprocal dendrodendritic synapses between glutamatergic mitral cell (MC) projection neurons and GABAergic granule cell (GC) interneurons in the accessory olfactory bulb (AOB). Although noradrenaline (NA) plays a critical role in the formation of the memory, the mechanism by which it exerts this effect remains unclear. Here we used extracellular field potential and whole-cell patch-clamp recordings to assess the actions of bath-applied NA (10 µM) on the glutamatergic transmission and its plasticity at the MC-to-GC synapse in the AOB...
April 2018: Learning & Memory
Nandkishor R Kotagale, Mir Touseef Ali, Chandrabhan T Chopde, Milind J Umekar, Brijesh G Taksande
Nicotine abstinence following chronic exposure is associated with impairments in memory and variety of cognitive functions. Daily nicotine (2 mg/kg, sc, four times daily) administration for 14 days and its abrupt withdrawal significantly impaired avoidance learning in inhibitory avoidance task as indicated by a significant decrease in the step through latency. Animals injected with agmatine (10-40 μg/rat, icv) from day 7 to 14 before the first daily dose of nicotine (2 mg/kg, sc) showed increased step through latencies during retrieval test...
March 10, 2018: Pharmacology, Biochemistry, and Behavior
Travis T Mallard, James R Ashenhurst, K Paige Harden, Kim Fromme
GABRA2, the gene encoding the α2 subunit of the GABAA receptor, potentially plays a role in the etiology of problematic drinking, as GABRA2 genotype has been associated with subjective response to alcohol and other alcohol-related reward processes. The GABRA2 gene has also been associated with illicit drug use, but the extent to which associations with drug use are independent of associations with alcohol use remains unclear, partly because most previous research has used a cross-sectional design that cannot discriminate comorbidity at the between-person level and co-occurrence within-persons...
February 2018: Journal of Abnormal Psychology
Dilara Nemutlu Samur, Rana Arslan, Sule Aydın, Nurcan Bektas
The purpose of this study is to assess the possible anti-allodynic and antihyperalgesic effect of valnoctamide, an amide derivative of valproic acid, at the doses of 40, 70 and 100mg/kg (i.p.) in neuropathic pain model induced by chronic constriction injury in rats, by using dynamic plantar test and plantar test (Hargreaves method), and to evaluate that the possible role of certain serotonin, noradrenergic, opioid and GABAergic receptors by pre-treatment with 1mg/kg (i.p.) ketanserin, yohimbine, naloxone and 0...
March 6, 2018: European Journal of Pharmacology
Cristiana Garisto, Zaccaria Ricci, Lorenzo Tofani, Simona Benegni, Chiara Pezzella, Paola Cogo
BACKGROUND: Dexmedetomidine is a selective agonist of α2 receptors that induces hypnotic, sedative and mild analgesic effect. The aim of our study was to test the effects of dexmedetomidine in combination with opioids and benzodiazepines compared to benzodiazepine-opioids alone. METHODS: A randomized controlled trial was conducted. Patients (children >30 days and <24 months undergoing correction of complex congenital heart diseases -CHD-) were randomized to receive 0...
March 7, 2018: Minerva Anestesiologica
Lingyan Wu, Lina Zhang, Bohan Li, Haowen Jiang, Yanan Duan, Zhifu Xie, Lin Shuai, Jia Li, Jingya Li
Obesity occurs when excess energy accumulates in white adipose tissue (WAT), whereas brown adipose tissue (BAT), which is specialized in dissipating energy through thermogenesis, potently counteracts obesity. White adipocytes can be converted to thermogenic "brown-like" cells (beige cells; WAT browning) under various stimuli, such as cold exposure. AMP-activated protein kinase (AMPK) is a crucial energy sensor that regulates energy metabolism in multiple tissues. However, the role of AMPK in adipose tissue function, especially in the WAT browning process, is not fully understood...
2018: Frontiers in Physiology
Myeong-Joo Kim, Ye-Ji Lee, Young-So Yoon, Jae H Lim, Eun-Mi Park, Young H Chong, Jihee Lee Kang
BACKGROUND/AIMS: The signal transducer and activator of transcription 6 (STAT6) transcription factor mediates PPARγ-regulated gene expression in macrophages. However, it remains largely unknown how proximal membrane signaling events initiated by apoptotic cell recognition upregulate PPARγ expression and activate the lung homeostatic program. METHODS: The STAT6 inhibitor AS1517499 was used to determine the role of STAT6 in mediating PPARγ activity, anti-inflammatory effects, and anti-fibrotic effects induced by apoptotic cell instillation after bleomycin treatment into C57BL/6 mice...
February 28, 2018: Cellular Physiology and Biochemistry
Hongli Chen, Xiaotong Sun, Xiaomei Yang, Yonghao Hou, Xiaoqian Yu, Yang Wang, Jianbo Wu, Dejie Liu, Huanliang Wang, Jingui Yu, Wenbo Yi
Mechanical ventilation (MV) may lead to ventilator-induced lung injury (VILI). Previous research has shown that dexmedetomidine attenuates pulmonary inflammation caused by MV, but the underlying mechanisms remain unclear. Our study aims to test whether dexmedetomidine has a protective effect against VILI and to explore the possible molecular mechanisms using the rat model. Thirty adult male Wistar rats weighing 200-250 g were randomly assigned to 5 groups (n = 6): control, low tidal volume MV (LMV), high tidal volume (HVT) MV (HMV), HVT MV + dexmedetomidine (DEX), HVT MV + dexmedetomidine + yohimbine (DEX+Y)...
February 20, 2018: Bosnian Journal of Basic Medical Sciences
Pooja Tajpara, Christopher Schuster, Elisabeth Schön, Philip Kienzl, Martin Vierhapper, Michael Mildner, Adelheid Elbe-Bürger
Together with keratinocytes (KCs) and the dense network of Langerhans cells (LCs), the epidermis is an ideal portal for vaccine delivery. Pattern recognition receptor agonists, in particular polyinosinic-polycytidylic acid [p(I:C)], are promising adjuvant candidates for therapeutic vaccination to generate protective T-cell immunity. Here we established an ex vivo skin explant model to study the expression and activation of double-stranded RNA (dsRNA)-sensing pattern recognition receptors in LCs and KCs in human skin...
March 6, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
Landon M Klein, Nicholas V Cozzi, Paul F Daley, Simon D Brandt, Adam L Halberstadt
Substantial effort has been devoted toward understanding the psychopharmacological effects of tryptamine hallucinogens, which are thought to be mediated by activation of 5-HT2A and 5-HT1A receptors. Recently, several psychoactive tryptamines based on the N,N-diallyltryptamine (DALT) scaffold have been encountered as recreational drugs. Despite the apparent widespread use of DALT derivatives in humans, little is known about their pharmacological properties. We compared the binding affinities of DALT and its 2-phenyl-, 4-acetoxy-, 4-hydroxy-, 5-methoxy-, 5-methoxy-2-methyl-, 5-fluoro-, 5-fluoro-2-methyl-, 5-bromo-, and 7-ethyl-derivatives at 45 receptor and transporter binding sites...
February 27, 2018: Neuropharmacology
Yuichiro Nishida, Minako Iyadomi, Hirotaka Tominaga, Hiroaki Taniguchi, Yasuki Higaki, Hiroaki Tanaka, Chisato Shimanoe, Megumi Hara, Keitaro Tanaka
The purpose of the current study was to examine the influence of single-nucleotide polymorphisms (SNPs) in the peroxisome proliferator-activated receptor-δ (PPAR-δ), PPAR-γ, and α2 isoforms of the catalytic subunit of AMP-activated protein kinase (PRKAA2) on the extent of changes in anthropometric indices and blood measurements through exercise-centered lifestyle intervention in middle-aged men. A total of 109 Japanese middle-aged male subjects (47.0 ± 0.4 years) participated in the baseline health checkup, 6-month exercise-centered lifestyle intervention, and second checkup conducted several months after the subject completed the intervention...
March 1, 2018: International Journal of Molecular Sciences
Wenjie Peng, Kim M Bouwman, Ryan McBride, Oliver C Grant, Robert J Woods, Monique H Verheije, James C Paulson, Robert P de Vries
All human influenza pandemics have originated from avian influenza viruses. Although multiple changes are needed for an avian virus to be able to transmit between humans, binding to human-type receptors is essential. Several research groups have reported mutations in H5N1 viruses that exhibit specificity to human-type receptors and promote respiratory droplet transmission between ferrets. Upon detailed analysis we have found that these mutants exhibit significant differences in fine receptor specificity compared to human H1N1 and H3N2 and retain avian-type receptor binding...
February 28, 2018: Journal of Virology
Andrea Kwakowsky, Beatriz Calvo-Flores Guzmán, Madhavi Pandya, Clinton Turner, Henry J Waldvogel, Richard L Faull
Gamma-aminobutyric acid (GABA) is the primary inhibitory neurotransmitter in the central nervous system. GABA type A receptors (GABAA Rs) are severely affected in Alzheimer's disease (AD). However, the distribution and subunit composition of GABAA Rs in the AD brain are not well understood. This is the first comprehensive study to show brain region- and cell layer-specific alterations in the expression of the GABAA R subunits α1-3, α5, β1-3 and γ2 in the human AD hippocampus, entorhinal cortex and superior temporal gyrus (STG)...
February 27, 2018: Journal of Neurochemistry
Patrick Grenier, David Wiercigroch, Mary C Olmstead, Catherine M Cahill
Long-term use of opioid analgesics is limited by tolerance development and undesirable adverse effects. Paradoxically, spinal administration of ultra-low-dose (ULD) G-protein-coupled receptor antagonists attenuates analgesic tolerance. Here, we determined whether systemic ULD α2-adrenergic receptor (AR) antagonists attenuate the development of morphine tolerance, whether these effects extend to the cannabinoid (CB1) receptor system, and if behavioral effects are reflected in changes in opioid-induced spinal gliosis...
February 23, 2018: Behavioural Pharmacology
Fumiya Shinohara, Yuta Asaoka, Hironori Kamii, Masabumi Minami, Katsuyuki Kaneda
Effects of stress on the reward system are well established in the literature. Although previous studies have revealed that stress can reinstate extinguished addictive behaviors related to cocaine, the effects of stress on the rewarding memory of cocaine are not fully understood. Here, we provide evidence that stress potentiates the expression of rewarding memory of cocaine via the activation of brainstem-reward circuitry using a cocaine-induced conditioned place preference (CPP) paradigm combined with restraint stress in rats...
February 26, 2018: Addiction Biology
Vikas Menon, Pravallika Madhavapuri
Mirtazapine is a novel tetracyclic antidepressant which enhances noradrenergic and serotonergic transmission by blocking central α2-adrenergic auto- and hetero-receptors. Due to favorable safety and adverse effect profile, it is often viewed as a promising agent for treatment of depression. Particularly, its anxiolytic and sleep-improving properties have led to its favorable positioning for the management of depression with insomnia. Our objective is to describe a case of depression with treatment-emergent nightmares induced by mirtazapine...
October 2017: Journal of Pharmacology & Pharmacotherapeutics
Yann S Mineur, Emma L Cahuzac, Tenna N Mose, Matthew P Bentham, Margreet E Plantenga, David C Thompson, Marina R Picciotto
Medications that target the noradrenergic system are important therapeutics for depression and anxiety disorders. More recently, clinical studies have shown that the α2-noradrenergic receptor (α2AR) agonist guanfacine can decrease stress-induced smoking relapse during acute abstinence, suggesting that targeting the noradrenergic system may aid in smoking cessation through effects on stress pathways in the brain. Acetylcholine (ACh), like the nicotine in tobacco, acts at nicotinic acetylcholine receptors (nAChRs) to regulate behaviors related to anxiety and depression...
February 22, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
Meijuan Liu, Huijuan Zhu, Yufei Dai, Hui Pan, Naishi Li, Linjie Wang, Hongbo Yang, Kemin Yan, Fengying Gong
Zinc-α2-glycoprotein (ZAG) plays an important role in the regulation of body weight, body fat, and glucose metabolism. In this study, we first measured ZAG levels in serum and ZAG mRNA levels in subcutaneous white adipose tissue (sWAT) among overweight/obese patients and lean control subjects. Second, we investigated the effects of ZAG administration on the body weight, body fat and glucose metabolism of high-fat diet (HFD)-induced obese ICR mice and the possible mechanisms involved. The results showed that serum ZAG and mRNA levels in sWAT were significantly decreased in overweight/obese patients and that both showed a negative association with body mass index (BMI) and body weight after adjustment for age and sex...
2018: Frontiers in Physiology
Eun-Hyo Cho, Mahmoud Soliman, Mia Madel Alfajaro, Ji-Yun Kim, Ja-Young Seo, Jun-Gyu Park, Deok-Song Kim, Yeong-Bin Baek, Mun-Il Kang, Sang-Ik Park, Jacques Le Pendu, Kyoung-Oh Cho
Some viruses within the Caliciviridae family initiate their replication cycle by attachment to cell surface carbohydrate moieties, histo-blood group antigens (HBGAs) and/or terminal sialic acids (SAs). Although bovine nebovirus (BNeV), one of the enteric caliciviruses, is an important causative agent of acute gastroenteritis in cattle, its attachment factors and possibly other cellular receptors remain unknown. Using a comprehensive series of protein-ligand biochemical assays, we sought to determine whether BNeV recognizes cell surface HBGAs and/or SAs as attachment factors...
February 21, 2018: Journal of Virology
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