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Several cholinesterase inhibitors have also been radiolabell
2021-07-20
Several cholinesterase inhibitors have also been radiolabelled with 11C as potential cholinesterase imaging agents. These include 11C-donepezil, 11C-methyltacrine, and 11C-physostigmine, which also have had limited success in demonstrating the known histochemically defined cholinesterase distributio
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Epitope analyses of AT AA
2021-07-20
Epitope analyses of AT1-AA and ET-AA indicate that the L 012 sodium salt of both autoantibodies are located at the second extracelluar loop of both receptors. The specific epitopes for both autoantibodies are similar to what was reported previously in a cohort of patients from Brazil [6] and for AT
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Tibolone is also efficacious on bone in
2021-07-20
Tibolone is also efficacious on bone in elderly women and induces a clear reduction in bone turnover markers [50], [51]. Rymer et al. showed that, after 10 years of treatment with tibolone, the difference in bone mineral density compared with a placebo group was more than 12% for both lumbar spine a
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Data on optimal hormone formulations routes of administratio
2021-07-20
Data on optimal hormone formulations, routes of administration, doses and duration of hormone use in young women with POF are lacking (Box 1). Transdermal tandospirone administration, which avoids the first-pass hepatic circulation and the increase in inflammatory markers such as C-reactive protein
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I bungarotoxin competes with ACh an endogenous activator
2021-07-19
[125I] α-bungarotoxin competes with ACh, an endogenous activator of α7-nACh receptors by binding to the ACh binding site on the receptor (Albuquerque et al., 2009). For this reason, the effect of curcumin was investigated on the specific binding of [125I] α-bungarotoxin. Saturation curves for the bi
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When six chemical inhibitors were incubated with TRB or TRC
2021-07-19
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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In the past few years neuroprotection via GLP
2021-07-19
In the past few years, neuroprotection via GLP-1R activation has been shown in several animal models of stroke, Alzheimer's, Parkinson's, Huntington's, ALS and traumatic TMC647055 Choline salt sale injury. This research field is rapidly growing and several reviews have been recently published (Darsa
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Mutation in BRCT II domain W
2021-07-19
Mutation in BRCT-II domain (W893R) either in the full-length context or the C-terminal context greatly reduced the expression of LIG4 (Fig. 2B, Fig. 3B), suggesting the importance of BRCT-II domain in the maintenance of LIG4. In this regard, it might be noted that LIG4 protein was undetectable in Li
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DGK is distributed exclusively in the brain particularly in
2021-07-19
DGKβ [9] is distributed exclusively in the brain, particularly in the striatum, cerebral cortex, olfactory bulb, and hippocampus [9,10]. This isozyme accumulates at the perisynaptic sites of medium spiny neurons in the striatum [11]. The 2 hydroxypropyl β cyclodextrin australia of DGKβ rapidly incr
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The authors gratefully acknowledge financial support from th
2021-07-19
The authors gratefully acknowledge financial support from the State of São Paulo Research Foundation (FAPESP, Fundação de Amparo à Pesquisa do Estado de São Paulo), grants 2013/07600-3 and 2013/25658-9, and the National Council for Scientific and Technological Development (CNPq, Conselho Nacional de
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Cys LT have been shown to be critical for
2021-07-19
Cys-LT have been shown to be critical for stimulation of monocytes to produce various proinflammatory factors [32,67]. Fig. 3 shows results obtained with human peripheral monocyte-derived macrophages differentiated for 6 days with 20 ng/ml macrophage colony-stimulating factor (M-CSF) and challenged
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The use of inhibitors clearly has its caveats and
2021-07-19
The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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The data correlations from Multiflash and DIPPR were used fo
2021-07-19
The data correlations from Multiflash™ [43] and DIPPR [44] were used for the liquid volume and heat of vaporization. For vapour pressure the curves were regressed from the experimental data present on both the DIPPR [44] and TRC [45] databases. As for liquid heat capacities both the latter databases
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This structure guided the variation of the
2021-07-19
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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ITF2357 mg More recently it was discovered that BChE hydroly
2021-07-19
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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