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mct2 inhibitor br Methods br Transfollicular penetration of
2022-01-13
Methods Transfollicular penetration of herbs and their active constituents used for hair loss treatment The transfollicular administration of pharmacologically active molecules is recognised as a significant element for therapeutic interest, mainly with regard to delivery to specific sites of
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Based on the results of compound appeared
2022-01-13
Based on the results of , NU 9056 synthesis appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while analogs and we
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As disclosed in our preceding paper
2022-01-13
As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, gtpase lacks an essent
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GPR agonistic activity was evaluated for the
2022-01-13
GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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br Reactive Dicarbonyls and Mitochondrial Dysfunction Althou
2022-01-13
Reactive Dicarbonyls and Mitochondrial Dysfunction Although mitochondrial dysfunction has been suggested to be one of the main pathogenic mechanisms in diabetic neuropathy, little is known about the nature and extent of mitochondrial damage resulting from chronic hyperglycemia. Mitochondria funct
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br Conflicts of interest br
2022-01-13
Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty
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br Conclusion br Conflict of Interest
2022-01-12
Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant
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br Introduction G protein coupled receptors GPCRs
2022-01-12
Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign
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Although it is well documented that FAAH substrates can elic
2022-01-12
Although it is well documented that FAAH substrates can elicit analgesic effects [for review see [47,48] and that systemic poly I:C administration induces mechanical allodynia in rats [14], to our knowledge this is the first study to demonstrate that enhancing FAAH substrate levels can modulate TLR3
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P7C3 In the next set of experiments we sought to
2022-01-12
In the next set of experiments, we sought to determine the source of lysosomal P7C3 inhibition by oxidative stress. Lysosomal exocytosis probably involves multiple steps including vesicle positioning, delivery, docking and fusion. The previous evidence and data in Fig. 1C,D show that TRPML1 is criti
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In studies described earlier IRL was administered
2022-01-12
In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat
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The synthesis of substituted pyrimidinone carboxamides is ou
2022-01-12
The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of N-(p-amylcinnamoyl) provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to affor
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Amyloid Beta-peptide (25-35) br Histamine H R Many of the hi
2022-01-12
Histamine H3R Many of the highlight H3R ligands have been described as suitable pharmacological tools for in vitro or in vivo studies and are designated here. The number of ligands and structural categories is huge, and a number of inclusive reviews of the SAR and properties of H3R ligands have b
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br Materials and methods br
2022-01-12
Materials and methods Results We examined the cardiac mitochondrial density of HKI and markers of oxidative and metabolic stress in trout exposed to an aerated control exposure, an aerated (normoxic) thermal insult, or a hyperoxic thermal insult. Should mtHK provide a cardioprotective effect i
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There has been some debate about
2022-01-12
There has been some debate about which types of liver cells might be able to activate canonical Hh signalling during liver injury. These uncertainties reflect technical challenges imposed by imperfect and inconsistent reagent specificity and the nature of the signalling process itself, which is quit
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