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Since the cloning of ARs
2023-10-19

Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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sVRPs were more sensitive to ABT than MSRs This result
2023-10-19

sVRPs were more sensitive to ABT-702 than MSRs. This result agrees with previous reports that the activation of A1 receptors more potently inhibits sVRPs than MSRs (Nakamura et al., 1997, Otsuguro et al., 2009). Importantly, sVRPs are thought to reflex C-fiber-evoked nociceptive transmission. Nocice
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In this study we make the first simultaneous
2023-10-19

In this study, we make the first simultaneous recordings of adenosine receptor agonist release in multiple brain regions at a temporal resolution less than 1 s. One of the most striking findings is that acetylcholine release has a remarkably similar temporal profile in the mPFC and dHPC, suggesting
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To date more than different
2023-10-19

To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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We have previously shown that the antinociceptive effect of
2023-10-19

We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific corticotropin releasing factor blockade or activation (Rojas-Corrales et al
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HT receptors are distributed throughout the brain within
2023-10-19

5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and DCC-2036 (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Bufton et al.
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In agreement with the role of
2023-10-19

In agreement with the role of ACLY in induced macrophage, we observe a drastically reduction of PGE2 levels when ACLY activity is inhibited. This is possible because PGE2 production requires arachidonic acid, which in turn is synthesized by elongation of dietary linoleic 1423 mg with acetyl-CoA pro
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The LOX hydroxide metabolites are
2023-10-19

The 15-LOX hydroxide metabolites are converted to secondary lipid mediators such as lipoxin A4 from 15-HETE and protectin D1/resolvin D1 from 17-HDoHE [45] (Fig. S3). Importantly, all of these secondary lipid mediators have anti-inflammatory and pro-resolving properties [46], [47], [48]. Lipoxin A4
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To the best of our knowledge there have
2023-10-18

To the best of our knowledge, there have been only a few reports on antiangiogenic activities about C. sanki, and its antiangiogenic constituents as well as its mechanism of action are worthy of further exploring and studying. Therefore, we carried out a bioassay-guided investigation of C. sanki in
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Insulin is the central hormone involved in the
2023-10-18

Insulin is the central hormone involved in the control of glucose and lipid metabolism. Other nonmetabolic effects of insulin are intensively studied as well. Activation of insulin receptor not only promotes glucose uptake, protein synthesis, and inhibits lipid metabolism, but also is crucial for re
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The increased occurrence of ARIA E in
2023-10-18

The increased occurrence of ARIA-E in APOE ε4 carriers in phase 2 studies resulted in separate protocols for carriers and noncarriers in the subsequent phase 3 studies. Two 18-month trials comprising 1121 carriers and 1331 noncarriers with mild to moderate AD tested doses of bapineuzumab that varied
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MAPs require divalent transition metal ions as
2023-10-18

MAPs require divalent transition metal ions as cofactors for activity [21]. Previous studies on MAPs from different organisms indicate cobalt ions to be the most preferred divalent metal activator [22]. However, MAPs also exhibit activity with other divalent cations like Mn(II), Ca(II), Ni(II) or Fe
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Recently two distinct small molecule inhibitors of PHGDH wer
2023-10-18

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Vanoxerine dihydrochloride with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM,
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Liao and van Linden et al divided the
2023-10-18

Liao [47] and van Linden et al. [48] divided the gap between the N-terminal and C-terminal lobes into a front cleft or pocket, a gate area, and a back cleft. The back pocket corresponds to the gate area and the back cleft. The front cleft includes the Gly-rich loop, the hinge, the linker connecting
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br Materials and methods br
2023-10-18

Materials and methods Results Discussion In the present study, we identified HBP1 as a novel substrate of AKT. This was demonstrated by in vitro phosphorylation assays and western blotting using phosphosite-specific antibodies. Three sites were identified by mass spectrometry and mutagenesi
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