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α2 receptor

Kwong-Fai Wong, Angela M Liu, Wanjin Hong, Zhi Xu, John M Luk
The Hippo pathway regulates the down-stream target Yes-associated protein (YAP) to maintain organ homeostasis, which is commonly inactivated in many types of cancers. However, how cell adhesion dysregulates the Hippo pathway activating YAP oncogene in hepatocellular carcinoma (HCC) remains unclear. Our findings demonstrate that α2β1 integrin (but not other β1 integrins) expressed in HCC cells, after binding to collagen extracellular matrix, could inhibit MST1 kinase phosphorylation and activate YAP pro-oncogenic activities...
October 19, 2016: Oncotarget
Mark J Millan, Jean-Michel Rivet, Alain Gobert
The highly-interconnected and neurochemically-rich frontal cortex plays a crucial role in the regulation of mood and cognition, domains disrupted in depression and other central nervous system disorders, and it is an important site of action for their therapeutic control. For improving our understanding of the function and dysfunction of the frontal cortex, and for identifying improved treatments, quantification of extracellular pools of neuromodulators by microdialysis in freely-moving rodents has proven indispensable...
October 17, 2016: Journal of Psychopharmacology
Lauren Luhrs, Cynthia Manlapaz, Karen Kedzie, Sandhya Rao, Sara Cabrera-Ghayouri, John Donello, Daniel Gil
Noradrenergic signaling, through the α2A and α2C adrenergic receptors modulates the cognitive and behavioral symptoms of disorders such as schizophrenia, attention deficit hyperactivity disorder (ADHD), and addiction. However, it is unknown whether the α2B receptor has any significant role in CNS function. The present study elucidates the potential role of the α2B receptor in CNS function via the discovery and use of the first subtype selective α2B antagonist (AGN-209419), and behavioral analyses of α-receptor KO mice...
October 14, 2016: Neuroscience
Srikanth Ravisankar, Devon Kuehn, Reese H Clark, Rachel G Greenberg, P Brian Smith, Christoph P Hornik
BACKGROUND: Systemic hypertension is increasingly recognised in premature infants. There is limited evidence regarding treatment, and most published treatment recommendations are based solely on expert opinions. METHODS: We identified all infants born ⩽32 weeks of gestation and ⩽1500 g birth weight discharged from one of 348 neonatal ICUs managed by the Pediatrix Medical Group between 1997 and 2013. We defined antihypertensive drugs as vasodilators, angiotensin-converting enzyme inhibitors, β receptor blockers, calcium channel blockers, and central α2 receptor agonists...
October 17, 2016: Cardiology in the Young
Janet C Tait, Evan W Mercer, Lucie Gerber, George N Robertson, William S Marshall
In eurythermic vertebrates, acclimation to the cold may produce changes in physiological control systems. We hypothesize that relatively direct osmosensitive control will operate better than adrenergic receptor mediated control of ion transport in cold vs. warm conditions. Fish were acclimated to full strength seawater (SW) at 21°C and 5°C for four weeks, gill samples and blood were taken and opercular epithelia mounted in Ussing style chambers. Short-circuit current (Isc) at 21°C and 5°C (measured at acclimation temperature), was significantly inhibited by the α2-adrenergic agonist clonidine but the ED50 dose was significantly higher in cold conditions (93...
October 13, 2016: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
Majid Motaghinejad, Manijeh Motevalian, Behnaz Shabab
Neurodegeneration induced by methylphenidate (MPH), as a central stimulant with unknown long-term consequences, in adult rats' brain and the possible mechanisms involved were studied. Rats were acutely treated with MPH in presence and absence of some receptor antagonists such as ketamine, topiramate, yohimibine and haloperidol. Motor activity and anxiety level in rats were monitored. Anti-oxidant and inflammatory parameters were also measured in isolated hippocampus and cerebral cortex. MPH treated groups (10 and 20 mg/kg) demonstrated anxiety-like behavior and increased motor activity...
October 14, 2016: Fundamental & Clinical Pharmacology
Daiki Yamanaka, Takashi Kawano, Atsushi Nishigaki, Bun Aoyama, Hiroki Tateiwa, Marie Shigematsu-Locatelli, Fabricio M Locatelli, Masataka Yokoyama
PURPOSE: In the present study, we examined whether and by what mechanisms dexmedetomidine (DMED) prevents the development of systemic inflammation (SI)-induced cognitive dysfunction in aged rats. METHODS: Animals received a single intraperitoneal (i.p.) injection of either 5.0 mg/kg lipopolysaccharide (LPS) or vehicle. LPS-treated rats were further divided into three groups: early DMED, late DMED, or midazolam (MDZ) treatment (n = 12 each). Seven days after LPS injection, cognitive function was evaluated using a novel object recognition task, followed by measurement of hippocampal levels of proinflammatory cytokines and Toll-like receptor 4 (TLR-4) expression...
October 13, 2016: Journal of Anesthesia
Renan B Ferreira, Mariana G de Oliveira, Edson Antunes, Wanda P Almeida, Badr M Ibrahim, Abdel A Abdel-Rahman
2-Aminothiazolines share an isosteric relationship with imidazolines and oxazolines with antihypertensive activity mainly mediated by the imidazoline I1-receptor. In the present work, we have prepared five aminothiazolines, following a previously described synthetic pathway. Aminothiazolines derived from dicyclopropylmethylamine (ATZ1) and cyclohexylamine (3) are unprecedented in the literature. Competitive radioligand assay was carried out with all synthetic compounds, and the I1 receptor affinity in comparison to rilmenidine in PC12 cells was determined...
October 8, 2016: European Journal of Pharmacology
Emily L Newman, Georgia Gunner, Polly Huynh, Darrel Gachette, Stephen J Moss, Trevor G Smart, Uwe Rudolph, Joseph F DeBold, Klaus A Miczek
BACKGROUND: Alcohol use disorders are associated with single-nucleotide polymorphisms in GABRA2, the gene encoding the GABAA receptor α2-subunit in humans. Deficient GABAergic functioning is linked to impulse control disorders, intermittent explosive disorder, and to drug abuse and dependence, yet it remains unclear whether α2-containing GABAA receptor sensitivity to endogenous ligands is involved in excessive alcohol drinking. METHODS: Male wild-type (Wt) C57BL/6J and point-mutated mice rendered insensitive to GABAergic modulation by benzodiazepines (BZD; H101R), allopregnanolone (ALLO) or tetrahydrodeoxycorticosterone (THDOC; Q241M), or high concentrations of ethanol (EtOH) (S270H/L277A) at α2-containing GABAA receptors were assessed for their binge-like, moderate, or escalated chronic drinking using drinking in the dark, continuous access (CA) and intermittent access (IA) to alcohol protocols, respectively...
September 26, 2016: Alcoholism, Clinical and Experimental Research
Qurrat U Ain, Robert M Owen, Kiyoyuki Omoto, Rubben Torella, Krishna C Bulusu, David C Pryde, Robert C Glen, Julian E Fuchs, Andreas Bender
Selective modulators of the γ-amino butyric acid (GABAA) family of receptors have the potential to treat a range of disease states related to cognition, pain and anxiety. While the development of various α subunit-selective modulators is currently underway for the treatment of anxiety disorders, the mechanistic understanding of the correlation between their bioactivity and efficacy, based on ligand-target interactions, is currently still lacking. In order to alleviate this situation, in the current study we have analyzed, using ligand-based and structure-based methods, a dataset of 5,440 GABAA modulators...
October 5, 2016: Molecular Pharmaceutics
Donald W Lee, Hung-Lun Hsu, Kaitlyn B Bacon, Susan Daniel
With the development of single-particle tracking (SPT) microscopy and host membrane mimics called supported lipid bilayers (SLBs), stochastic virus-membrane binding interactions can be studied in depth while maintaining control over host receptor type and concentration. However, several experimental design challenges and quantitative image analysis limitations prevent the widespread use of this approach. One main challenge of SPT studies is the low signal-to-noise ratio of SPT videos, which is sometimes inevitable due to small particle sizes, low quantum yield of fluorescent dyes, and photobleaching...
2016: PloS One
Anna Maria Waszkielewicz, Kubacka Monika, Pańczyk Katarzyna, Mogilski Szczepan, Siwek Agata, Głuch-Lutwin Monika, Gryboś Anna, Filipek Barbara
In the search for new hypotensive agents some new aroxyalkyl or aroxyethoxyethyl derivatives of piperazine have been synthesized and evaluated for their pharmacological properties. Pharmacological tests included receptor binding assays toward adrenergic receptors α1, α2 and β1, additionally 5-HT1A, functional bioassay and in vivo evaluation of hypotensive activity as well as antidepressant-like potential. All the tested compounds exhibited α1-antagonistic properties, three of them possessed also hypotensive activity in rats...
September 15, 2016: Bioorganic & Medicinal Chemistry Letters
Makoto Sato, Takayuki Kunisawa, Atsushi Kurosawa, Tomoki Sasakawa
STUDY OBJECTIVE: Hypertension or hypotension in patients receiving continuous infusions of dexmedetomidine (DEX) is often due to changes in vascular resistance caused by α2 receptor stimulation. We investigated whether baseline perfusion index (PI) and pleth variability index (PVI), derived from pulse oximetry readings, could predict DEX-induced changes in the hemodynamic status in spontaneously breathing patients. DESIGN: Observational study. SETTING: Operating room...
November 2016: Journal of Clinical Anesthesia
Bradley K Taylor, Karin N Westlund
Central noradrenergic centers such as the locus coeruleus (LC) are traditionally viewed as pain inhibitory; however, complex interactions among brainstem pathways and their receptors modulate both inhibition and facilitation of pain. In addition to the well-described role of descending pontospinal pathways that inhibit spinal nociceptive transmission, an emerging body of research now indicates that noradrenergic neurons in the LC and their terminals in the dorsal reticular nucleus (DRt), medial prefrontal cortex (mPFC), spinal dorsal horn, and spinal trigeminal nucleus caudalis participate in the development and maintenance of allodynia and hyperalgesia after nerve injury...
September 29, 2016: Journal of Neuroscience Research
Jianshen Chai, Li Luo, Fengyan Hou, Xia Fan, Jing Yu, Wei Ma, Wangqi Tang, Xue Yang, Junyu Zhu, Wenyuan Kang, Jun Yan, Huaping Liang
Macrophages are key responders of inflammation and are closely related with oxidative stress. Activated macrophages can enhance oxygen depletion, which causes an overproduction of reactive oxygen species (ROS) and leads to further excessive inflammatory response and tissue damage. Agmatine, an endogenous metabolite of L-arginine, has recently been shown to have neuroprotective effects based on its antioxidant properties. However, the antioxidant effects of agmatine in peripheral tissues and cells, especially macrophages, remain unclear...
2016: PloS One
Zhen Qin, Jing-Jing Wan, Yang Sun, Peng-Yuan Wang, Ding-Feng Su, Hong Lei, Xia Liu
We found previously that acute phase protein orosomucoid reacts to fatigue and activates C-C chemokine receptor type 5 to increase muscle glycogen storage and enhance muscle endurance (Lei et al., 2016). To explore the underlying molecular mechanisms, we investigated the role of AMP-activated protein kinase, a critical fuel sensor in skeletal muscle, in C-C chemokine receptor type 5-mediated orosomucoid action. It was found orosomucoid increased skeletal muscle AMP-activated protein kinase activation in a time- and dose- dependent manner, which was largely prevented by pharmacological blocking or knockout of C-C chemokine receptor type 5...
2016: Frontiers in Pharmacology
E V Navolotskaya, D V Zinchenko, Y A Zolotarev, A A Kolobov, V M Lipkin
The synthetic peptide LKEKK corresponding to sequence 16-20 of human thymosin-α1 and 131-135 of human interferon-α2 was labeled with tritium to specific activity 28 Ci/mol. The [3H]LKEKK bound with high affinity (Kd = 3.7 ± 0.3 nM) to donor blood T-lymphocytes. Treatment of cells with trypsin or proteinase K did not abolish [3H]LKEKK binding, suggesting the non-protein nature of the peptide receptor. The binding was inhibited by thymosin-α1, interferon-α2, and cholera toxin B subunit (Ki = 2.0 ± 0.3, 2...
August 2016: Biochemistry. Biokhimii︠a︡
Shawn David O'Connor, Omar Hoseá Cabrera, Joseph D Dougherty, Sukrit Singh, Brant Stephen Swiney, Patricia Salinas-Contreras, Nuri Bradford Farber, Kevin Kiyoshi Noguchi
OBJECTIVES: Glucocorticoids (GC) are used to improve respiratory mechanics in preterm infants despite clinical evidence linking neonatal GC therapy to cerebellar pathology. In developing mouse cerebellum, the GC dexamethasone (DEX) causes rapid GC-induced neural progenitor cell apoptosis (GINA). Focusing on pharmacological neuroprotection strategies, we investigated whether dexmedetomidine (DMT) protects against GINA. METHODS: Neonatal mice were pretreated with DMT prior to DEX challenge...
September 27, 2016: Journal of Maternal-fetal & Neonatal Medicine
Marie Kubota, Kaoru Takeuchi, Shumpei Watanabe, Shinji Ohno, Rei Matsuoka, Daisuke Kohda, Shin-Ichi Nakakita, Hiroaki Hiramatsu, Yasuo Suzuki, Tetsuo Nakayama, Tohru Terada, Kentaro Shimizu, Nobutaka Shimizu, Mitsunori Shiroishi, Yusuke Yanagi, Takao Hashiguchi
Mumps virus (MuV) remains an important pathogen worldwide, causing epidemic parotitis, orchitis, meningitis, and encephalitis. Here we show that MuV preferentially uses a trisaccharide containing α2,3-linked sialic acid in unbranched sugar chains as a receptor. Crystal structures of the MuV attachment protein hemagglutinin-neuraminidase (MuV-HN) alone and in complex with the α2,3-sialylated trisaccharide revealed that in addition to the interaction between the MuV-HN active site residues and sialic acid, other residues, including an aromatic residue, stabilize the third sugar of the trisaccharide...
October 11, 2016: Proceedings of the National Academy of Sciences of the United States of America
Elise Kleeman, Sakura Nakauchi, Hailing Su, Richard Dang, Marcelo A Wood, Katumi Sumikawa
Children of mothers who smoked during pregnancy are at significantly greater risk for cognitive impairments including memory deficits, but the mechanisms underlying this effect remain to be understood. In rodent models of smoking during pregnancy, early postnatal nicotine exposure results in impaired long-term hippocampus-dependent memory, functional loss of α2-containing nicotinic acetylcholine receptors (α2(∗) nAChRs) in oriens-lacunosum moleculare (OLM) cells, increased CA1 network excitation, and unexpected facilitation of long-term potentiation (LTP) at Schaffer collateral-CA1 synapses...
September 19, 2016: Neurobiology of Learning and Memory
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