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Other N substituted carboxamide oxy pyridine derivatives a h
2022-03-18
Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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br Conclusions br Introduction Astrocytes
2022-03-18
Conclusions Introduction Astrocytes contribute to physiological OG-L002 function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with energy substra
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br Pharmacology br Background to GPR function br
2022-03-18
Pharmacology Background to GPR35 function The emerging function of GPR35 in the nervous system Conclusions The role of GPR35 in the modulation of synaptic transmission, neurogenic and inflammatory pain, and potential signalling pathways involved in these processes are beginning to emerge
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As part of our discovery
2022-03-18
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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We suggest that the FRET enhancement observed when the
2022-03-18
We suggest that the FRET enhancement observed when the modified mD1 protein containing Acd at position 28 was excited at 260nm (), may differ from the diminution in fluorescence observed following excitation at 280nm due to the excitation of different transitions in Trp (i.e., the L and L transition
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br Results br Discussion The twin cysteine motif is
2022-03-18
Results Discussion The twin-cysteine motif is an evolutionary conserved motif in all primate lentiviruses except HIV-1 and some strains of SIVcpz according to sequence analysis (Bohl et al., 2013). It is assumed that only those SIVcpz which have lost the twin-cysteines successfully evolved to
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BCCA occlusion followed by reperfusion
2022-03-18
BCCA occlusion, followed by reperfusion injury, significantly increased the brain AT1 and AT2 receptor expression in mice. Reports have demonstrated elevation of AT1 receptor expression in the cerebral 891 during ischemia [34,35]. The gene expression of brain AT2 receptor is increased in both in vi
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We recently reported the first cyclopropene analog
2022-03-18
We recently reported the first cyclopropene-analog of the amino APETx2 neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [28]. We obt
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Several studies have shown that regulation of glutamate
2022-03-18
Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upregu
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For another the N terminal sequence of native glucagon is
2022-03-17
For another, the N-terminal sequence of native glucagon is highly conserved, and positions 8, 9, 16 and 18 are noteworthy in maintaining glucagon activity [18], [20], [21]. It also achieves a degree of selectivity from its C-terminal residues, and a significant contribution is made by the C-terminal
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Multiple mechanisms have been suggested by which glucagon ca
2022-03-17
Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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Formoterol Hemifumarate Importantly bioelectric circuits in
2022-03-17
(4) Importantly, bioelectric circuits in tissues (Fig. 2A) have a capacity to store long-term patterning information. An example is planarian anterior-posterior patterning: during regeneration, each fragment cut from a worm needs to build a head and tail at their correct ends. This process is regula
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Galanin a amino acid peptide was first isolated in from
2022-03-17
Galanin, a 29/30-amino-acid peptide, was first isolated in 1983 from porcine intestine by Tatemoto and collaborators [70]. It is widely distributed throughout the central and peripheral nervous systems as well as other tissues. It is involved in a wide range of physiological functions, such as modul
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First identified in as the
2022-03-17
First identified in 1982 as the second mammalian glutathione peroxidase [23], we and Stockwell's group demonstrated in 2014 that the selenoperoxidase GPX4 is the key upstream regulator of ferroptosis [12], [13]. The role of GPX4 as the main regulator in the ferroptotic process is based on its unique
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We characterized the enzyme corresponding to
2022-03-17
We characterized the enzyme corresponding to N1. FPP was the most effective substrate as allylic diphosphate, and the activities with GPP and DMAPP were 50% and 11% that with FPP, respectively. The analysis of the prenols resulting from the treatment of prenyl diphosphates with Closantel Sodium mg
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