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enfuvirtide Utilization of fascinating properties such as lo
2022-03-30
Utilization of fascinating properties, such as localized surface plasmon resonance (LSPR), high fluorescent quantum yield, biocompatible nature, chromogenic and electrocatalytic functionality of several nanomaterials for histamine sensing is also quite evident where the nanomaterials have served as
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br Introduction Local anesthetics LAs are a
2022-03-30
Introduction Local anesthetics (LAs) are a set of common medicines used for pain management in clinical settings. Up to now, LAs have been extensively used for peripheral nerve blocks, interventional spinal procedures, and epidural anesthesia [1]. In addition to their anesthetic and analgesic eff
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A series of P P ureas were explored first
2022-03-30
A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen Topiroxostat receptor of the urea yielded , a molecule which retained intrinsic
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A 61603 hydrobromide receptor The GLU Epac transgenic mouse
2022-03-29
The GLU-Epac transgenic mouse enabled us to monitor cAMP responses to GPR119 ligands in individual primary cultured L-cells. Not all L-cells were found to be responsive to AR231453, suggesting there may be a subpopulation of L-cells that do not express functional GPR119. There was a tendency for sma
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br Introduction Over the past two decades the prevalence
2022-03-29
Introduction Over the past two decades, the prevalence of obesity and obesity-associated metabolic diseases, such as T2D, insulin resistance, atherosclerosis and stroke, have been dramatically increased globally [1], [2], and obesity has been suggested to be the leading cause of the reduced life
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Finally we investigated if calpain truncation affects GlyT t
2022-03-29
Finally, we investigated if calpain truncation affects GlyT1 turnover and trafficking. To simulate calpain cleavage at the T602/T603 and G626/S627 sites we constructed GlyT1 transporters missing the last 12 and 36 amino acids. Since the 36 amino PF-573228 truncation also removes all C-terminal anti
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Due to the high structural
2022-03-29
Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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Hexamethonium Bromide Previous studies have demonstrated tha
2022-03-29
Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio
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Introduction l Glutamate is a
2022-03-29
Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is
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Tail group SAR of the imidazole
2022-03-29
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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br Dysregulation of glutamate transporter expression and fun
2022-03-29
Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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Ionotropic glutamate receptors GluRs are ligand gated
2022-03-29
Ionotropic glutamate receptors (GluRs) are ligand-gated ion channels that mediate information processing at the majority of excitatory synapses in the brain and participate in such physiological processes as learning and memory, development and maintenance of cellular connections, and pain perceptio
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br Introduction The alternative splicing of
2022-03-29
Introduction The alternative splicing of pre-mRNA is essential for generating multiple matured mRNAs from a single gene by selectively removing introns. Neural pp3 show many examples of regulated alternative splicing events, which produce structural changes in proteins important for the developme
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br Introduction Anthocyanidins and anthocyanins glycosides o
2022-03-29
Introduction Anthocyanidins and anthocyanins (glycosides of anthocyanidins) are flavonoid phenolic compounds that are among the most common types of plant pigments [1]. They typically are responsible for the red, orange, blue, and violet colors in flowers, fruits, and vegetative tissues [1], [2].
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Here we used chemogenetic modulation of MBH
2022-03-29
Here, we used chemogenetic modulation of MBH GHSR neurons to address the role of the endogenous ghrelin system in the normal, hyperphagic response to a short-term fast. Studies demonstrating the requirement of an intact ghrelin-GHSR system for the rebound food intake following fasting have been inco
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