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Skeletal pain associated with bone
2024-12-19
Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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It is well known that neurosteroids such
2024-12-19
It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls
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(+)-MK 801 Maleate Aconitase clusters are prone to oxidation
2024-12-19
Aconitase clusters are prone to oxidations and are among the first to undergo a change in transition state during stages of electrophilic stress rendering them inactive [31]. Aconitase activity in LETO and OLETF did not differ at T0 suggesting that the early onset of insulin resistance may not be at
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Other reports however have indicated that
2024-12-19
Other reports, however, have indicated that all components of RAS are produced within the central nervous system (CNS) (Saavedra, 2005). Thus, AGTR1 and AGTR2 in circumventricular organs and in cerebrovascular endothelial cells may respond to circulating ANG2 of peripheral origin, whereas neural rec
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Gratifyingly compound also demonstrated improved physicochem
2024-12-18
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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RVX-208 receptor br Role of OCT in histamine clearance Hista
2024-12-18
Role of OCT3 in histamine clearance Histamine is a powerful neuromodulator, as well as a regulator of immune processes and vascular tone in the central nervous system (Gross, 1981; Haas et al., 2008; Jutel et al., 2006). In contrast to 5-HT and the catecholamines, a high-affinity transporter for
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A clear link between ADR stimulation and
2024-12-18
A clear link between α2-ADR stimulation and decreased respiration in β-cells is established and consistent with proteomics data. Current discoveries in islets have identified physical interactions between ADR-coupled G proteins and cellular components such as insulin vesicles and ion channels (Zhao
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Adenosine is an endogenous nucleoside that plays
2024-12-18
Adenosine is an endogenous nucleoside that plays pivotal roles in different physiological and pathophysiological processes by triggering specific cell-surface receptors both in the ctep synthesis and in the periphery. The adenosine receptors (ARs) are four different subtypes of G protein-coupled re
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To assess relative metabolic activity and proliferation of
2024-12-18
To assess relative metabolic activity and proliferation of Cy7 carboxylic acid (non-sulfonated) australia attached to various substrates we used the MTT assay [29], [30]. In order to compare the metabolic activity of cells under the various conditions irrespective of the number or viability of the
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Until now the molecular interactions of Tmod or Lmod with
2024-12-18
Until now, the molecular interactions of Tmod or Lmod with wst-1 assay had been assessed in pyrene-actin polymerization assays [13], [23], [27], [28], [44], [45] or directly measured using non-denaturing polyacrylamide gel-electrophoresis (for Tmod isoforms only [23]), ITC (for Tmod1 and Lmod2) [43
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Argatroban br Results and discussion br Conclusion In summar
2024-12-18
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic Argatroban group extending from the C-3 position of the aniline and substituted grou
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br Conflicts of interest br Introduction
2024-12-18
Conflicts of interest Introduction Phosphatidic Picroside II receptor phosphatase (PAP) enzymes are responsible for catalyzing the reaction that dephosphorylates phosphatidic acid (PA), which in turn produces diacylglycerol (DAG) and a phosphate group during phospholipid regulation (Fig. 1A) [
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br Conclusion This is the first report to
2024-12-18
Conclusion This is the first report to show that treatment of lung cancer cell lines, A549 and H1299, with ovatodiolid stimulates intracellular reactive oxygen species generation and induces DNA damage. Subsequently activates ATM/ATR and CHK1/2 signaling pathway, inhibits CDC25C and p21WAF1/CIP1,
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23401 zip code br Conclusion This is the first report to
2024-12-18
Conclusion This is the first report to show that treatment of lung cancer cell lines, A549 and H1299, with ovatodiolid stimulates intracellular reactive oxygen species generation and induces DNA damage. Subsequently activates ATM/ATR and CHK1/2 signaling pathway, inhibits CDC25C and p21WAF1/CIP1,
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The enzyme Arginase ARG plays a role in
2024-12-18
The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],
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