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Compounds and were evaluated for their pharmacokinetic prope
2021-09-09

Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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All of the designed compounds was synth http
2021-09-09

All of the designed compounds – was synthesized from -cyclopropane aldehyde , which was prepared following a procedure we reported previously. Treatment of with 4-chlorobenzene-1,2-diamine in pyridine constructed benzimidazole structure of , which was subjected to deprotection and subsequent oxidat
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Although no data exist on Ptc gene expression in
2021-09-09

Although no data exist on Ptc52 gene MAPK Inhibitor Library in other plant species, the expression pattern presented in this study shows perceptibly low levels of transcript accumulation in tomato seeds and roots, low levels in the stem, flower and green fruit, and high levels in the leaves. This c
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The selection of mutations in vivo with
2021-09-09

The selection of mutations in vivo with antivirals is a complex process involving, among other things, the frequency of a given mutation prior to treatment, the effect of that mutation on viral protein function, and the interplay of a given mutation pattern with host immune mechanisms. Investigation
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Metallothioneins MTs that are intracellular proteins respons
2021-09-09

Metallothioneins (MTs) that are intracellular proteins responsible for the maintenance of metal homeostasis are involved in arsenic toxicity (Kita et al., 2006). Four major MT isoforms have been reported so far, MT1, MT2A, MT3 and MT4. The synthesis of MT1 and MT2A isoforms in mammal cells can be in
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While published data around the functional significance of G
2021-09-08

While published data around the functional significance of GPR84 are quite sparse, details of signaling pathways initiated by the receptor are even more limited, including in recombinant systems. In recombinant cells, GPR84 activation reportedly leads to Gi pathway activation, resulting in pertussis
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br Synthetic Antagonists for FFA To date only compounds
2021-09-08

Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this
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Although we showed that RBL H Sc cells took
2021-09-08

Although we showed that RBL-2H3 Sc98 ache inhibitor took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including
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PD 0325901 In respect of clinical development Takeda has
2021-09-08

In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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A number of experimental data declare a tight interdependenc
2021-09-08

A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in SB742457 mg and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Behari and Shrivastav
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bupropion hydrochloride synthesis With the advent of genome
2021-09-08

With the advent of genome sequencing, hexokinase gene sequences are now available from a far greater number of vertebrate species, as well as from diverse non-vertebrate animal species. As indicated above, searches of vertebrate genome sequences revealed the existence of a novel fifth member of the
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br Introduction The growth hormone secretagogue receptor GHS
2021-09-08

Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt
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Since our new compound Fex could be a new
2021-09-08

Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 DMAP with transwell experiments. From and , we fou
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br Results br Discussion Previous studies have
2021-09-07

Results Discussion Previous studies have shown that all the components of ET system are expressed by various neuronal and non-neuronal structures throughout the CNS (McCumber et al., 1990; Giaid et al., 1991). In effect, endothelin-converting enzyme activity, mRNA, ET-1 and ET-3 immunoreactivi
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On the other hand G
2021-09-07

On the other hand, G9a/GLP could also alter neuronal function without directly altering the transcription level of particular plasticity-related protein: the consolidation of early-LTP to late-LTP, as well as the reversal of mGluR-LTD by G9a/GLP inhibition required PKMζ translation and its downstrea
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