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galanin receptor

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https://www.readbyqxmd.com/read/28720509/the-neuropeptide-galanin-promotes-an-anti-thrombotic-phenotype-on-endocardial-endothelial-cells-from-heart-failure-patients
#1
Christina Tyrrell, Amanda Toyooka, Faiza Khan, Kent L Thornburg, James O Mudd, Wohaib Hasan
Thromboembolic complications are a significant cause of mortality and re-hospitalization in heart failure (HF) patients. One source of thrombi is the ventricular endocardial surface that becomes increasingly pro-thrombotic as HF progresses. Anticoagulation comes with bleeding risks so identifying therapeutic agents for improving cardiac endothelial health are of critical clinical importance. Endocardial endothelial cells are closely apposed to cardiac sympathetic nerves. In HF, cardiac sympathetic nerves are dysregulated and promote disease progression...
July 12, 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/28648499/light-dependent-regulation-of-sleep-and-wake-states-by-prokineticin-2-in-zebrafish
#2
Shijia Chen, Sabine Reichert, Chanpreet Singh, Grigorios Oikonomou, Jason Rihel, David A Prober
Light affects sleep and wake behaviors by providing an indirect cue that entrains circadian rhythms and also by inducing a direct and rapid regulation of behavior. While circadian entrainment by light is well characterized at the molecular level, mechanisms that underlie the direct effect of light on behavior are largely unknown. In zebrafish, a diurnal vertebrate, we found that both overexpression and mutation of the neuropeptide prokineticin 2 (Prok2) affect sleep and wake behaviors in a light-dependent but circadian-independent manner...
July 5, 2017: Neuron
https://www.readbyqxmd.com/read/28636888/responsiveness-of-pituitary-to-galanin-throughout-the-reproductive-cycle-of-male-european-sea-bass-dicentrarchus-labrax
#3
P Pinto, Z Velez, C Sousa, S Santos, A Andrade, M V Alvarado, A Felip, S Zanuy, A V M Canário
The neuropeptide galanin (Gal) is a putative factor regulating puberty onset and reproduction through its actions on the pituitary. The present study investigated the pituitary responsiveness to galanin and the patterns of galanin receptors (Galrs) expression throughout the reproductive cycle of two years old male European sea bass (Dicentrarchus labrax), an important aquaculture species. Quantitative analysis of pituitary and hypothalamus transcript expression of four galr subtypes revealed differential regulation according to the testicular developmental stage, with an overall decrease in expression from the immature stage to the mid-recrudescence stage...
June 19, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28580231/hormones-and-neuropeptide-receptor-heteromers-in-the-ventral-tegmental-area-targets-for-the-treatment-of-loss-of-control-of-food-intake-and-substance-use-disorders
#4
REVIEW
Sergi Ferré
Hormones and neuropeptides represent biological correlates of internal homeostatic signals detected and integrated in the hypothalamus, which establishes a robust functional connection with the ventral tegmental area (VTA). The hypothalamus-VTA connection determines the ability of these signals to influence central dopaminergic neurotransmission and, therefore, their ability to increase responsiveness to their reward-associated stimuli and to establish appropriate associative learning. The hypothalamus also provides the main source of the multiple neuropeptides that are released in the VTA...
2017: Current Treatment Options in Psychiatry
https://www.readbyqxmd.com/read/28540352/dataset-on-galanin-receptor-3-mutants-that-improve-recombinant-receptor-expression-and-stability-in-an-agonist-and-antagonist-bound-form
#5
Thao T Ho, Jasmine T Nguyen, Juping Liu, Pawel Stanczak, Aaron A Thompson, Yingzhuo G Yan, Jasmine Chen, Charles K Allerston, Charles L Dillard, Hao Xu, Nicholas J Shoger, Jill S Cameron, Mark E Massari, Kathleen Aertgeerts
Galanin Receptor 3 (GALR3) is a G-protein-coupled receptor with a widespread distribution in the brain and plays a role in a variety of physiologic processes including cognition/memory, sensory/pain processing, hormone secretion, and feeding behavior. Therefore, GALR3 is considered an attractive CNS drug target (Freimann et al., 2015) [1]. This dataset contains GALR3 point mutants that improve recombinant protein expression and thermal stability of the receptor contained in virus-like particles (VLPs) or obtained by detergent-purification of baculovirus-infected insect cells...
June 2017: Data in Brief
https://www.readbyqxmd.com/read/28525358/galanin-suppresses-proliferation-of-human-u251-and-t98g-glioma-cells-via-its-subtype-1-receptor
#6
REVIEW
Zhu Mei, Yutao Yang, Yun Li, Feiya Yang, Junfa Li, Nianzeng Xing, Zhi-Qing David Xu
Galanin is a neuropeptide with a widespread distribution throughout the nervous and endocrine systems, and recent studies have shown an anti-proliferative effect of galanin on several types of tumors. However, whether and how galanin and its receptors are involved in the regulation of cell proliferation in glioma cells remains unclear. In this study, the roles of galanin and its subtype 1 receptor (GAL1) in the proliferation of human U251 and T98G glioma cells were investigated. We found that galanin significantly suppressed the proliferation of U251 and T98G cells as well as tumor growth in nude mice...
June 15, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/28434790/short-n-terminal-galanin-fragments-are-occurring-naturally-in-vivo
#7
Robert Ihnatko, Elvar Theodorsson
The galanin family currently consists of four peptides, namely galanin, galanin-message associated peptide, galanin-like peptide and alarin. Unlike galanin that signals through three different G protein-coupled receptors; GAL1, GAL2, and GAL3, binding at its N-terminal end, the cognate receptors for other members of the galanin family are currently unknown. Research using short N-terminal galanin fragments generated either by enzymatic cleavage or solid-phase synthesis has revealed differences in their receptor binding properties exerting numerous biological effects distinct from galanin(1-29) itself...
April 7, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28431685/galr3-mediates-galanin-proliferative-effects-on-postnatal-hippocampal-precursors
#8
D Khan, M Khan, Johan Runesson, M Zaben, W P Gray
Galanin, a neuropeptide co-released from noradrenergic and serotonergic projection neurons to the dentate gyrus, has recently emerged as an important mediator for signaling neuronal activity to the subgranular neurogenic stem cell niche supporting adult hippocampal neurogenesis. Galanin and its receptors appear to play key roles in depression-like behavior, and effects on hippocampal neurogenesis are relevant to pharmacological strategies for treating depression, which in part appear to rely on restoring altered neurogenesis...
April 5, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28422162/a-comparative-analysis-of-human-and-mouse-islet-g-protein-coupled-receptor-expression
#9
Stefan Amisten, Patricio Atanes, Ross Hawkes, Inmaculada Ruz-Maldonado, Bo Liu, Fariborz Parandeh, Min Zhao, Guo Cai Huang, Albert Salehi, Shanta J Persaud
G-protein coupled receptors (GPCRs) are essential for islet function, but most studies use rodent islets due to limited human islet availability. We have systematically compared the GPCR mRNA expression in human and mouse islets to determine to what extent mouse islets can be used as surrogates for human islets to study islet GPCR function, and we have identified species-specific expression of several GPCRs. The A3 receptor (ADORA3) was expressed only in mouse islets and the A3 agonist MRS 5698 inhibited glucose-induced insulin secretion from mouse islets, with no effect on human islets...
April 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28382595/preclinical-analgesic-and-safety-evaluation-of-the-galr2-preferring-analog-nax-810-2
#10
Cameron S Metcalf, Misty D Smith, Brian D Klein, Daniel R McDougle, Liuyin Zhang, Grzegorz Bulaj
The potential clinical utility of galanin peptidic analogs has been hindered by poor metabolic stability, lack of brain penetration, and hyperglycemia. In addition to possessing potent anticonvulsant efficacy, galanin analogs are analgesic in various assays. The purpose of these studies was to evaluate the lead galanin receptor type 2 (GalR2)-preferring analog, NAX 810-2, in various pain assays, as well as determine any potential for insulin inhibition, growth hormone stimulation, and cognitive impairment. NAX 810-2 was evaluated in mouse (carrageenan, formalin, tail flick, plantar incision) and rat pain models (partial sciatic nerve ligation)...
July 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28378856/involvement-of-galanin-and-galanin-receptor-2-in-nociceptive-modulation-in-anterior-cingulate-cortex-of-normal-rats-and-rats-with-mononeuropathy
#11
Meng-Lin Zhang, Hong-Bo Wang, Feng-Hua Fu, Long-Chuan Yu
The present study was performed to explore the role of galanin and galanin receptor 2 in nociceptive modulation in anterior cingulate cortex (ACC) of normal rats and rats with mononeuropathy. Intra-ACC injection of galanin induced significant increases in hindpaw withdrawal latencies (HWLs) to thermal and mechanical stimulations in both normal rats and rats with mononeuropathy, the increased HWLs were attenuated significantly by intra-ACC injection of galanin receptor 2 antagonist M871, indicating an involvement of galanin receptor 2 in nociceptive modulation in ACC...
April 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28288814/galanin-1-15-enhancement-of-the-behavioral-effects-of-fluoxetine-in-the-forced-swimming-test-gives-a-new-therapeutic-strategy-against-depression
#12
Antonio Flores-Burgess, Carmelo Millón, Belén Gago, Manuel Narváez, Dasiel O Borroto-Escuela, Guadalupe Mengod, José Angel Narváez, Kjell Fuxe, Luis Santín, Zaida Díaz-Cabiale
The pharmacological treatment of major depression is mainly based on drugs elevating serotonergic (5-HT) activity. Specifically, selective 5-HT reuptake inhibitors, including Fluoxetine (FLX), are the most commonly used for treatment of major depression. However, the understanding of the mechanism of action of FLX beyond its effect of elevating 5-HT is limited. The interaction between serotoninergic system and neuropeptides signaling could be a key aspect. We examined the ability of the neuropeptide Galanin(1-15) [GAL(1-15)] to modulate the behavioral effects of FLX in the forced swimming test (FST) and studied feasible molecular mechanisms...
May 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28274821/the-galanin-3-receptor-antagonist-snap-37889-suppresses-alcohol-drinking-and-morphine-self-administration-in-mice
#13
Karlene J Scheller, Spencer J Williams, Andrew J Lawrence, Elvan Djouma
The neuropeptide, galanin, is widely expressed in the central and peripheral nervous systems and is involved in a range of different functions including nociception, neurogenesis, hormone release, reproduction, cognitive function and appetite. Given the overlap between galanin expression and reward circuitry in the brain, galanin has been targeted for alcohol use disorder (AUD) and opioid dependency. Furthermore, the galanin-3 receptor (GAL3) specifically regulates emotional states and plays a role in motivation, reward and drug-seeking behaviour...
May 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28270751/understanding-the-role-of-gpcr-heteroreceptor-complexes-in-modulating-the-brain-networks-in-health-and-disease
#14
REVIEW
Dasiel O Borroto-Escuela, Jens Carlsson, Patricia Ambrogini, Manuel Narváez, Karolina Wydra, Alexander O Tarakanov, Xiang Li, Carmelo Millón, Luca Ferraro, Riccardo Cuppini, Sergio Tanganelli, Fang Liu, Malgorzata Filip, Zaida Diaz-Cabiale, Kjell Fuxe
The introduction of allosteric receptor-receptor interactions in G protein-coupled receptor (GPCR) heteroreceptor complexes of the central nervous system (CNS) gave a new dimension to brain integration and neuropsychopharmacology. The molecular basis of learning and memory was proposed to be based on the reorganization of the homo- and heteroreceptor complexes in the postjunctional membrane of synapses. Long-term memory may be created by the transformation of parts of the heteroreceptor complexes into unique transcription factors which can lead to the formation of specific adapter proteins...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28203483/galanin-protects-from-caspase-8-12-initiated-neuronal-apoptosis-in-the-ischemic-mouse-brain-via-galr1
#15
Yun Li, Zhu Mei, Shuiqiao Liu, Tong Wang, Hui Li, Xiao-Xiao Li, Song Han, Yutao Yang, Junfa Li, Zhi-Qing David Xu
Galanin (GAL) plays key role in many pathophysiological processes, but its role in ischemic stroke remains unclear. Here, the models of 1 h middle cerebral artery occlusion (MCAO)/1-7 d reperfusion (R)-induced ischemic stroke and in vitro cell ischemia of 1 h oxygen-glucose deprivation (OGD)/24 h reoxygenation in primary cultured cortical neurons were used to explore GAL's effects and its underlying mechanisms. The results showed significant increases of GAL protein levels in the peri-infarct region (P) and infarct core (I) within 48 h R of MCAO mice (p<0...
February 2017: Aging and Disease
https://www.readbyqxmd.com/read/28196718/the-neuropeptide-galanin-is-up-regulated-during-cholestasis-and-contributes-to-cholangiocyte-proliferation
#16
Matthew McMillin, Gabriel Frampton, Stephanie Grant, Sharon DeMorrow
During the course of cholestatic liver diseases, mitotically dormant cholangiocytes proliferate and subsequently acquire a neuroendocrine phenotype. Galanin is a neuroendocrine factor responsible for regulation of physiological responses, such as feeding behavior and mood, and has been implicated in the development of fatty liver disease, although its role in biliary hyperplasia is unknown. Biliary hyperplasia was induced in rats via bile duct ligation (BDL) surgery, and galanin was increased in serum and liver homogenates from BDL rats...
April 2017: American Journal of Pathology
https://www.readbyqxmd.com/read/28196617/the-neuropeptides-galanin-and-galanin-1-15-in-depression-like-behaviours
#17
REVIEW
Carmelo Millón, Antonio Flores-Burgess, Manuel Narváez, Dasiel O Borroto-Escuela, Belén Gago, Luis Santín, Estela Castilla-Ortega, José Ángel Narváez, Kjell Fuxe, Zaida Díaz-Cabiale
Galanin is a 29 amino acid neuropeptide widely distributed in neurons within the central nervous system. Galanin exerts its biological activities through three different G protein-receptors and participates in a number of functions, including mood regulation. Not only Galanin but also Galanin N-terminal fragments like Galanin(1-15) are active at the central level. In this work, we review the latest findings in studies on Galanin and Galanin(1-15) in depression-related behaviours. Our focus is on animal models for depression, and we pay some attention to research data obtained in human studies...
January 31, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28178884/improved-post-thaw-function-and-epigenetic-changes-in-mesenchymal-stromal-cells-cryopreserved-using-multicomponent-osmolyte-solutions
#18
Kathryn Pollock, Rebekah M Samsonraj, Amel Dudakovic, Roman Thaler, Aron Stumbras, David H McKenna, Peter I Dosa, Andre J van Wijnen, Allison Hubel
Current methods for freezing mesenchymal stromal cells (MSCs) result in poor post-thaw function, which limits the clinical utility of these cells. This investigation develops a novel approach to preserve MSCs using combinations of sugars, sugar alcohols, and small-molecule additives. MSCs frozen using these solutions exhibit improved post-thaw attachment and a more normal alignment of the actin cytoskeleton compared to cells exposed to dimethylsulfoxide (DMSO). Osteogenic and chondrogenic differentiation assays show that cells retain their mesenchymal lineage properties...
June 1, 2017: Stem Cells and Development
https://www.readbyqxmd.com/read/28098336/preclinical-evaluation-of-intravenous-nax-810-2-a-novel-galr2-preferring-analog-for-anticonvulsant-efficacy-and-pharmacokinetics
#19
Cameron S Metcalf, Brian D Klein, Daniel R McDougle, Liuyin Zhang, Dan Kaufmann, Grzegorz Bulaj, H Steve White
OBJECTIVE: Potential clinical utility of galanin or peptidic analogs has been hindered by poor metabolic stability, lack of brain penetration, and hyperglycemia due to galanin receptor subtype 1 (GalR1) activation. NAX 810-2, a galanin receptor subtype 2 (GalR2)-preferring galanin analog, possesses 15-fold greater affinity for GalR2 over GalR1 and protects against seizures in the mouse 6 Hz, corneal kindling, and Frings audiogenic seizure models. The purpose of these studies was to further evaluate the preclinical efficacy and pharmacokinetics of NAX 810-2 in mice...
February 2017: Epilepsia
https://www.readbyqxmd.com/read/28079752/changes-in-dorsal-root-ganglion-gene-expression-in-response-to-spinal-cord-stimulation
#20
Dana M Tilley, David L Cedeño, Courtney A Kelley, Margaret DeMaegd, Ramsin Benyamin, Ricardo Vallejo
BACKGROUND AND OBJECTIVES: Spinal cord stimulation (SCS) has been shown to influence pain-related genes in the spinal cord directly under the stimulating electrodes. There is limited information regarding changes occurring at the dorsal root ganglion (DRG). This study evaluates gene expression in the DRG in response to SCS therapy. METHODS: Rats were randomized into experimental or control groups (n = 6 per group). Experimental animals underwent spared-nerve injury, implantation of lead, and continuous SCS (72 hours)...
March 2017: Regional Anesthesia and Pain Medicine
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