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https://www.readbyqxmd.com/read/28916379/carboxymethyl-fenugreek-galactomannan-gellan-gum-calcium-silicate-composite-beads-for-glimepiride-delivery
#1
Hriday Bera, Srilatha Mothe, Sabyasachi Maiti, Sridhar Vanga
Novel carboxymethyl fenugreek galactomannan (CFG)-gellan gum (GG)-calcium silicate (CS) composite beads were developed for controlled glimepiride (GLI) delivery. CFG having degree of carboxymethylation of 0.71 was synthesized and characterized by FTIR, DSC and XRD analyses. Subsequently, GLI-loaded hybrids were accomplished by ionotropic gelation technique employing Ca(+2)/Zn(+2)/Al(+3) ions as cross-linkers. All the formulations demonstrated excellent drug encapsulation efficiency (DEE, 48-97%) and sustained drug release behaviour (Q8h, 62-94%)...
September 12, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28912557/a-nmda-receptor-calcium-influx-assay-sensitive-to-stimulation-by-glutamate-and-glycine-d-serine
#2
Hongqiu Guo, L Miguel Camargo, Fred Yeboah, Mary Ellen Digan, Honglin Niu, Yue Pan, Stephan Reiling, Gilberto Soler-Llavina, Wilhelm A Weihofen, Hao-Ran Wang, Y Gopi Shanker, Travis Stams, Anke Bill
N-methyl-D-aspartate-receptors (NMDARs) are ionotropic glutamate receptors that function in synaptic transmission, plasticity and cognition. Malfunction of NMDARs has been implicated in a variety of nervous system disorders, making them attractive therapeutic targets. Overexpression of functional NMDAR in non-neuronal cells results in cell death by excitotoxicity, hindering the development of cell-based assays for NMDAR drug discovery. Here we report a plate-based, high-throughput approach to study NMDAR function...
September 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28912112/molecular-basis-of-peripheral-olfactory-sensing-during-oviposition-in-the-behavior-of-the-parasitic-wasp-anastatus-japonicus
#3
Yinliang Wang, Qi Chen, Junqi Guo, Jing Li, Jiatong Wang, Ming Wen, Hanbo Zhao, Bingzhong Ren
Anastatus japonicus is a parasitic wasp and natural enemy of the litchi pest Tessaratoma papillosa, and for decades in China, A. japonicus has been mass-reared inside the eggs of Antheraea pernyi to control T. papillosa. A series of experiments was performed to explore the olfactory mechanism underlying the oviposition behavior of A. japonicus. First, a transcriptomic analysis was performed on the antennae of A. japonicus, and the resulting assemblies led to the generation of 70,473 unigenes. Subsequently, 21,368 unigenes were matched to known proteins, 48 odorant receptors (ORs) (including Orco) and 13 antennal ionotropic receptors (IRs) (including the co-receptors IR8a and IR25a) were identified and predicted to form complete open reading frames (ORFs)...
September 11, 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28902515/theoretical-and-experimental-investigation-of-acidity-of-the-glutamate-receptor-antagonist-6-7-dinitro-1-4-dihydro-quinoxaline-2-3-dione-dnqx-and-its-possible-implication-in-glua2-binding
#4
Gutto Raffyson Silva de Freitas, Sara E Coelho, Norberto K V Monteiro, Jannyely Moreira Neri, Livia Nunes Cavalcanti, Josiel B Domingos, Davi S Vieira, Miguel A F de Souza, Fabrício G Menezes
The acidity of organic compounds is highly relevant to understanding several biological processes. Although the relevance and challenges in estimating pKa values of organic acids is recognized by several reported works in the literature, there is a lack in determining the acidity of amides. This paper presents an experimental/theoretical combined investigation on the acid dissociation of the compound 6,7-dinitro-1,4-dihydro-quinoxaline-2,3-dione (DNQX), a well-established antagonist of ionotropic glutamate receptor GluA2...
September 13, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28900300/rogdi-defines-gabaergic-control-of-a-wake-promoting-dopaminergic-pathway-to-sustain-sleep-in-drosophila
#5
Minjong Kim, Donghoon Jang, Eunseok Yoo, Yangkyun Oh, Jun Young Sonn, Jongbin Lee, Yoonhee Ki, Hyo Jin Son, Onyou Hwang, Changwook Lee, Chunghun Lim, Joonho Choe
Kohlschutter-Tönz syndrome (KTS) is a rare genetic disorder with neurological dysfunctions including seizure and intellectual impairment. Mutations at the Rogdi locus have been linked to development of KTS, yet the underlying mechanisms remain elusive. Here we demonstrate that a Drosophila homolog of Rogdi acts as a novel sleep-promoting factor by supporting a specific subset of gamma-aminobutyric acid (GABA) transmission. Rogdi mutant flies displayed insomnia-like behaviors accompanied by sleep fragmentation and delay in sleep initiation...
September 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28898645/sensory-neurobiology-wet-fly-fishing
#6
Elizabeth Marin, Marta Costa
A neuron responding to moist air and its ionotropic receptor have been identified in Drosophila melanogaster. Moreover, second-order neurons integrate temperature and humidity information before reaching higher brain centres.
September 11, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28894232/antennal-transcriptome-and-expression-analyses-of-olfactory-genes-in-the-sweetpotato-weevil-cylas-formicarius
#7
Shu-Ying Bin, Meng-Qiu Qu, Xin-Hua Pu, Zhong-Zhen Wu, Jin-Tian Lin
The sweetpotato weevil, Cylas formicarius (Fabricius), is a serious pest of sweetpotato. Olfaction-based approaches, such as use of synthetic sex pheromones to monitor populations and the bait-and-kill method to eliminate males, have been applied successfully for population management of C. formicarius. However, the molecular basis of olfaction in C. formicarius remains unknown. In this study, we produced antennal transcriptomes from males and females of C. formicarius using high-throughput sequencing to identify gene families associated with odorant detection...
September 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28891049/differential-projections-of-the-densocellular-and-intermediate-parts-of-the-hyperpallium-in-the-pigeon-columba-livia
#8
Yasuro Atoji, Sonjoy Sarkar, J Martin Wild
The visual Wulst in birds shows a four-layered structure: apical part of the hyperpallium (HA), interstitial part of HA (IHA), intercalated part of hyperpallium (HI), and densocellular part of hyperpallium (HD). HD also connects with the hippocampus and olfactory system. Because HD is subjacent to HI, the two have been treated as one structure in many studies, and the fiber connections of HD have been examined by afferents and efferents originating outside HD. However, to clarify the difference between these two layers, they need to be treated separately...
September 10, 2017: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/28889974/ionotropic-receptors-mediate-drosophila-oviposition-preference-through-sour-gustatory-receptor-neurons
#9
Yan Chen, Hubert Amrein
Carboxylic acids are present in many foods, being especially abundant in fruits. Yet, relatively little is known about how acids are detected by gustatory systems and whether they have a potential role in nutrition or provide other health benefits. Here we identify sour gustatory receptor neurons (GRNs) in tarsal taste sensilla of Drosophila melanogaster. We find that most tarsal sensilla harbor a sour GRN that is specifically activated by carboxylic and mineral acids but does not respond to sweet- and bitter-tasting chemicals or salt...
August 31, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28887453/hyaluronic-acid-based-extracellular-matrix-regulates-surface-expression-of-glun2b-containing-nmda-receptors
#10
Barbara Schweitzer, Jeet Singh, Anna Fejtova, Laurent Groc, Martin Heine, Renato Frischknecht
Cortical areas of the juvenile rodent brain display a high degree of structural and functional plasticity, which disappears later in development. Coincident with the decline of plasticity 1) the hyaluronic acid-based extracellular matrix (ECM) of the brain, which stabilizes synapses and neuronal circuit is formed and 2) N-methyl-D-aspartate subtype of ionotropic glutamate receptors (NMDARs) implied in synaptic plasticity switch from mainly GluN2B to GluN2A subunit-containing receptors. Here we tested the hypothesis that ECM influences the NMDAR subunit composition in dissociated neuronal cultures...
September 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28872835/revisiting-the-quinoxalinedione-scaffold-in-the-construction-of-new-ligands-for-the-ionotropic-glutamate-receptors
#11
Charles S Demmer, David Rombach, Na Liu, Birgitte Nielsen, Darryl S Pickering, Lennart Bunch
More than two decades ago, the quinoxalinedione scaffold was shown to act as an α-amino acid bioisoster. Following extensive structure-activity relationship (SAR) studies, the antagonists DNQX, CNQX, and NBQX in the ionotropic glutamate receptor field were identified. In this work, we revisit the quinoxalinedione scaffold and explore the incorporation of an acid functionality in the 6-position. The SAR studies disclose that by this strategy it was possible to tune in iGluR selectivity among the AMPA, NMDA, and KA receptors, and to some extent also obtain full receptor subtype selectivity...
September 5, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28870203/the-dlgap-family-neuronal-expression-function-and-role-in-brain-disorders
#12
REVIEW
Andreas H Rasmussen, Hanne B Rasmussen, Asli Silahtaroglu
The neurotransmitter glutamate facilitates neuronal signalling at excitatory synapses. Glutamate is released from the presynaptic membrane into the synaptic cleft. Across the synaptic cleft glutamate binds to both ion channels and metabotropic glutamate receptors at the postsynapse, which expedite downstream signalling in the neuron. The postsynaptic density, a highly specialized matrix, which is attached to the postsynaptic membrane, controls this downstream signalling. The postsynaptic density also resets the synapse after each synaptic firing...
September 4, 2017: Molecular Brain
https://www.readbyqxmd.com/read/28864032/in-memory-of-norman-bowery-1944-2016
#13
REVIEW
David G Trist, Terry P Kenakin, Thomas P Blackburn
This article is in memory of Professor Norman Bowery (1944-2016). Norman was a pharmacologist who spent most of his career researching the pharmacology of γ-aminobutyric acid (GABA). He discovered a novel metabotropic receptor subtype, GABAB, that is pharmacologically, and structurally different from the original ionotropic receptor now designated as GABAA. In his research he also studied the neurotransmitters glutamate and substance P, two molecules whose release in parts of the spinal cord is inhibited by baclofen a GABAB receptor agonist...
August 29, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/28863815/direct-interactions-of-cholesterol-with-pentameric-ligand-gated-ion-channels-testable-hypotheses-from-computational-predictions
#14
Grace Brannigan
Several essential ionotropic neurotransmitter receptors, including the nicotinic acetylcholine receptor (nAChR) and gamma-aminobutyric acid (GABA) type A receptor (GABAAr), belong to the family of pentameric ligand-gated ion channels (pLGICs). Function of these receptors is particularly sensitive to their lipid environment, including cholesterol and cholesterol-derived neurosteroids. Direct structural data investigating interactions between sterols and pLGICs, as well as their role in modulatory mechanisms, are largely unavailable...
2017: Current Topics in Membranes
https://www.readbyqxmd.com/read/28862072/intranasal-delivery-of-tapentadol-hydrochloride-loaded-chitosan-nanoparticles-formulation-characterization-and-its-in-vivo-evaluation
#15
Ankit Javia, Hetal Thakkar
The aim of the present investigation was to formulate Tapentadol Hydrochloride loaded chitosan nanoparticles (CS-NPs) for nose to brain delivery. Chitosan nanoparticles were prepared using ionotropic gelation technique. Optimization of the formulation and process parameters was done using Box-Behnken Design. The entrapment efficiency, drug loading, Z-average size and zeta potential of the optimized batch were 63.49±1.61%, 17.25±1.38%w/w, 201.2±1.5 nm and +49.3 mV respectively. In-vitro release study showed 84...
September 1, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28857341/the-multidimensional-ionotropic-receptors-of-drosophila-melanogaster
#16
REVIEW
S Rimal, Y Lee
Ionotropic receptors (IRs), which form ion channels, can be categorized into conserved 'antennal IRs', which define the first olfactory receptor family of insects, and species-specific 'divergent IRs', which are expressed in gustatory receptor neurones. These receptors are located primarily in cell bodies and dendrites, and are highly enriched in the tips of the dendritic terminals that convey sensory information to higher brain centres. Antennal IRs play important roles in odour and thermosensation, whereas divergent IRs are involved in other important biological processes such as taste sensation...
August 31, 2017: Insect Molecular Biology
https://www.readbyqxmd.com/read/28856684/selective-synaptic-connections-in-the-retinal-pathway-for-night-vision
#17
Deborah L Beaudoin, Mania Kupershtok, Jonathan B Demb
The mammalian retina encodes visual information in dim light using rod photoreceptors and a specialized circuit: rods→rod bipolar cells→AII amacrine cell. The AII amacrine cell uses sign-conserving electrical synapses to modulate ON cone bipolar cell terminals and sign-inverting chemical (glycinergic) synapses to modulate OFF cone cell bipolar terminals; these ON and OFF cone bipolar terminals then drive the output neurons, retinal ganglion cells (RGCs), following light increments and decrements, respectively...
August 30, 2017: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/28856174/a-rare-syndrome-of-grid2-deletion-in-2-siblings
#18
Aravindhan Veerapandiyan, Stephanie Enner, Venkatraman Thulasi, Xue Ming
The Glutamate receptor, ionotropic, delta 2 gene codes for an ionotropic glutamate delta-2 receptor, which is selectively expressed in cerebellar Purkinje cells, and facilitates cerebellar synapse organization and transmission. The phenotype associated with the deletion of Glutamate receptor, ionotropic, delta 2 gene in humans was initially defined in 2013. In this case report, the authors describe 2 brothers who presented with developmental delay, tonic upward gaze, nystagmus, oculomotor apraxia, hypotonia, hyperreflexia, and ataxia...
January 2017: Child neurology open
https://www.readbyqxmd.com/read/28837330/development-of-a-drug-delivery-system-based-on-chitosan-nanoparticles-for-oral-administration-of-interferon-%C3%AE
#19
Camila Cánepa, Julieta C Imperiale, Carolina A Berini, Marianela Lewicki, Alejandro Sosnik, Mirna M Biglione
Despite the good clinical efficacy of interferon-alpha (IFNα) to treat some types of cancer and viral infections, this biological drug is underused given its severe adverse effects and high dosing parenteral regimens. Aiming to achieve a breakthrough in therapy with IFNα, this work reports for the first time on the design and full characterization of a novel nanomedicine of IFNα-2b-loaded chitosan nanoparticles (IFN-CT NPs) for oral delivery. IFN-CT NPs produced by ionotropic gelation, encapsulating approximately 100% of the drug, showed a size of 36 ± 8 nm, zeta potential of +30 mV (dynamic light scattering), and spherical morphology (transmission electron microscopy)...
September 8, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28828501/access-to-the-odor-world-olfactory-receptors-and-their-role-for-signal-transduction-in-insects
#20
REVIEW
Joerg Fleischer, Pablo Pregitzer, Heinz Breer, Jürgen Krieger
The sense of smell enables insects to recognize and discriminate a broad range of volatile chemicals in their environment originating from prey, host plants and conspecifics. These olfactory cues are received by olfactory sensory neurons (OSNs) that relay information about food sources, oviposition sites and mates to the brain and thus elicit distinct odor-evoked behaviors. Research over the last decades has greatly advanced our knowledge concerning the molecular basis underlying the reception of odorous compounds and the mechanisms of signal transduction in OSNs...
August 21, 2017: Cellular and Molecular Life Sciences: CMLS
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