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The existence of EAAT subtypes raises obvious questions
2021-09-07

The existence of 5 EAAT subtypes raises obvious questions as to the cellular and anatomical distribution of the various transporters (for review, see Gegelashvili & Schousboe, 1998, Danbolt, 2001). While difference in techniques (i.e., protein vs. mRNA), reagents, and preparations (i.e., in vivo vs.
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ICH induced striatal lesion produced a reduction of EAAT exp
2021-09-07

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino AT7867 transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia (Ra
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Although the overall structures of mGlu and mGlu VFTs are
2021-09-07

Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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It is an aspiring task to apply the glutamate
2021-09-07

It is an aspiring task to apply the glutamate biosensor for in vivo measurements in Nicotine Difartrate tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in dia
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WZ3146 synthesis br Voltage dependent anion channel
2021-09-06

Voltage-dependent anion channel VDAC is a ubiquitous protein showing well conserved structural and functional properties in spite of major variations in its sequence (for review see [50]). Most of what we know about VDAC electrophysiological properties (for reviews, see [51], [52]) was initially
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Increasing trans epithelial transport efficiency is another
2021-09-06

Increasing trans-epithelial transport efficiency is another area where different strategies are being developed for overcoming transcytosis. Enhancing the affinity for the basal membrane and weakening apical exocytosis through the optimisation of surface hydrophobicity have been demonstrated [79]. S
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GSK has also been used as PET radiotracer
2021-09-06

GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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In various models histamine has been shown to
2021-09-06

In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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HER genotype was determined in breast cancer tissue of breas
2021-09-06

HER2 genotype was determined in breast cancer tissue of 73 breast cancer patients. As previously reported, Ile655Val and Ala1170Pro genotypes measured in breast cancer tissues were available for 71 and 69 breast cancer patients, respectively. Briefly, 77.5% (55/71) of patients were homozygous for th
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Three additional Type I CDK
2021-09-06

Three additional Type I CDK8 and CDK19 kinase inhibitors have also been recently reported. Orally available 3-benzylindazole 12 was discovered by optimization of compounds with HSP90 affinity to yield potent and selective CDK8 inhibitors. Compound 12 showed strong binding activity for CDK8 with an I
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It was revealed that various
2021-09-06

It was revealed that various injured or infected organs of Hippeastrum produce a mixture of an orange-colored chalcone and flavans which can be oxidized to red-colored dimer (Wilmowicz et al., 2014, Wink and Lehmann, 1996), preventing the penetration of injured tissues by Phoma narcissi, Botrytis ci
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Any brain damage including that caused by amyloid
2021-09-06

Any Nevirapine damage, including that caused by β-amyloid, triggers activation of microglia, the resident immune cells of the CNS. These cells cluster around amyloid plaques, in which they extend cytoplasmic processes (Combs, 2009). The significance of this response is controversial, but one possib
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LPCs have been previously described as potential
2021-09-06

LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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Several studies have found that GPR
2021-09-06

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Wang Resin expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Ri
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Z-LEHD-FMK GPR co localizes with ghrelin in the duodenum gus
2021-09-06

GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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