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An alternative approach to improving pharmacokinetic
2022-04-11
An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl
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Acknowledgements br Introduction The neurotransmitter glycin
2022-04-11
Acknowledgements Introduction The neurotransmitter glycine acts through two receptors: a strychnine-sensitive glycine receptor (GlyA) and a strychnine-insensitive glycine receptor (GlyB). GlyA is localized to the neuronal membrane post-synaptic to inhibitory glycinergic neurons, whereas GlyB is
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Four polymorphic variants of Neil namely S C rs G
2022-04-11
Four polymorphic variants of Neil1, namely, S82C (rs5745905), G83D (rs5745906), C136R (rs5745907) and D252N (rs5745926) were characterized by Roy et al. in 2007 (Table 1). Analyses of AP site incision on Tg containing oligonucleotide showed that S82C and D252N variants had wild type activity and car
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In insects structural cuticular proteins CPs play important
2022-04-11
In insects, structural cuticular proteins (CPs) play important roles in determining the diverse physical properties of the cuticle, depending on developmental stages, as well as different body regions, as a result of interactions with other CPs and the structural biopolymer chitin [4]. Many studies
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Lamina II SG spinal cord neurons play an important role
2022-04-11
Lamina II (SG) spinal cord neurons play an important role in regulating nociceptive input from the periphery [20,21]. Moreover, lamina II neurons are concentrated with glycinergic or GABAergic inhibitory interneurons. Therefore, it is possible that β-alanine might modulate nociceptive transmission i
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br Materials and methods br Results br Discussion
2022-04-11
Materials and methods Results Discussion l-glutamate is the major excitatory neurotransmitter in the brain, and is functionally involved in many processes of the nervous system which have been connected with several neurological diseases [4]. These conditions are characterized by the time-d
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A number of experimental data declare a tight interdependenc
2022-04-11
A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in TH588 and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Behari and Shrivastava, 20
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ATP is essential for maintaining the
2022-04-11
ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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br Materials and methods br Results Bgal from Alteromonas
2022-04-09
Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino 5 aza 2 deoxycytidine residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other ad
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In the present study the relative mRNA
2022-04-09
In the present study, the relative mRNA prostanoid levels of CsLCCH3 and Cs8916 subunits in the egg were the highest, which were consistent with those of LsLCCH3 and Ls8916 from L. striatellus (Wei et al., 2017b) and were also similar to CsRDLs (Sheng et al., 2018; Meng et al., 2018). Overall, the
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Natural product based drug discovery can be enhanced with
2022-04-09
Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in butein binding assays, we used molecular modeling to predict how well these compounds fit t
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Compared to a large database of NSCLC samples
2022-04-09
Compared to a large database of NSCLC samples matched for disease type, many of the frequently altered genes were similar to those seen in this series of FGFR fusion-positive samples; however, there were notable exceptions. As expected, alterations in known NSCLC drivers (KRAS and EGFR) were signifi
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br Conclusions Symptoms from bilateral
2022-04-09
Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhibi
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Finally the optimized leads and were tested
2022-04-09
Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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Consistent with a similar study
2022-04-09
Consistent with a similar study, we found economic status to be very important to domestic funding of HIV. Upper-middle-income and high-income countries are more likely to have fiscal space for health and be less reliant on external sources. Moreover, richer countries often attract larger cofinancin
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