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In addition researchers studying GPR
2022-06-29

In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it N1-Methylpseudo-UTP is unclear why Sanofi-Aventis chose to terminate collaboration with
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Capillary monolithic columns obtained by in situ
2022-06-29

Capillary monolithic columns obtained by in situ polymerization have been developed rapidly as an efficient chromatographic stationary phase, which exhibits excellent reproducibility, reliable stability and fast transfer kinetics [18]. Recently, it has been extensively applied in capillary liquid ch
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Results indicated that superfusion of orexin alone glutamate
2022-06-29

Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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Recent studies revealed that synthetic oligomeric A decrease
2022-06-29

Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast
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Here we studied the effects of
2022-06-29

Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si
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hcv protease inhibitor Peripheral injury or disease induced
2022-06-29

Peripheral injury- or disease-induced alterations in synaptic efficacy occur not only at the first synapse made by the primary nociceptive afferents in the spinal dorsal horn but are also operational in several regions processing the sensorimotor as well as emotional-affective components of pain, su
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Ethanol decreased the value of desensitization
2022-06-29

Ethanol decreased the τ-value of desensitization for GluR-Di. Coexpression of stargazin or γ4 further increased the effect of ethanol on desensitization (Fig. 3A, B). The highest ethanol concentration tested (200mM) reduced the τ-value by 16.5±4.9% (n=5) in the control receptors and by 29.3±9.3% (n=
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Limitations of our study are
2022-06-29

Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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However ghrelin has a short half life of min because
2022-06-29

However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr
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Despite a robust impact on
2022-06-29

Despite a robust impact on learned, social feeding behaviors, we observed no differences in body weight or food intake when the control or vHP GHSR-1A KD animals were maintained on either a normal chow diet or a Western diet high in fat and sugar. This is interesting in light of our previous work sh
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Analgesic activity was evaluated by measuring tail
2022-06-29

Analgesic activity was evaluated by measuring tail flick latencies to the immersion of rat’s tail in water, maintained at ∼51°C [18] after recovery from anesthesia. Typically, rats were immobilized inside a restrainer, leaving only the tail exposed, which was then immersed into the hot water bath, a
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Since we were able to reach low micromolar to
2022-06-29

Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr
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Prior models suggest that the terminal ends of the
2022-06-29

Prior models suggest that the terminal ends of the endocrine FGFs individually determine FGFR and KLB recognition, with little or no cross-talk. Our results confirm that short C-terminal sequences are necessary and sufficient to bind KLB and, supportive of a common mechanism, the underlying structur
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The ETB receptor has been shown to
2022-06-28

The ETB receptor has been shown to decrease sodium transport in the renal medullary collecting duct and medullary thick ascending limb of Henle10, 11, 12, 13, 18. However, both inhibitory and stimulatory effects of endothelin have been reported in the proximal tubule16, 47, 48, 49. In the rat, endot
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The molecular mechanism of gliotransmitter release is not fu
2022-06-28

The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular psoralen of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in glutamate release
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