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The results of cell culture models were further
2024-09-18
The results of cell culture models were further supported by in vivo studies in mice treated with PXR and/or AhR agonists, PCN and β-NF. In these mice, AhR-regulated cyp1a1, and cyp1a2 were suppressed by PXR activation as determined by real time Q-PCR (Fig. 3). The level of PXR mRNA was not changed
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In a recent series of
2024-09-18
In a recent series of studies from our laboratory, to characterize the contractile systems within the rat Azimilide wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist induced con
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The cellular mechanism underlying the CGS mediated inhibitio
2024-09-18
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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NLX a k a F or befiradol exhibits nanomolar
2024-09-18
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in histone methyltransferase to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Addi
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gsk3beta receptor br Introduction Epilepsy is characterized
2024-09-18
Introduction Epilepsy is characterized by spontaneous recurrent seizures and represents one of the most frequent neurological diseases affecting about 60 million people worldwide (McNamara, 1999). It is estimated that up to 50% of all cases are triggered by “initial precipitating injuries”, such
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br Materials and methods br Results br Discussion
2024-09-18
Materials and methods Results Discussion Recent studies have highlighted TCS 2002 and autophagy as novel targets for the treatment of liver fibrosis [7,14]. In this study, we demonstrated that catalpol protected the rat liver from CCl4-caused injury and fibrogenesis in vivo and in vitro for
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The amino hydroxy methyl isoxazolepropionic
2024-09-18
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic UNC669 (AMPA) receptor is also enriched in postsynaptic striatal neurons (Bernard et al., 1997, Kondo et al., 2000, Reimers et al., 2011). Its activity is subjected to the regulation by a mechanism involving phosphorylation (Lu and Roche, 2012). F
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We also showed that steatosis induced an additional increase
2024-09-18
We also showed that steatosis induced an additional increase of ASK1 activation that was associated to the exacerbation of hepatocyte and liver damage and was unrelated to ER stress. Indeed, several settings, also different to ER stress, can induce ASK1 activation and many of them involve oxidative
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In addition to attracting immune cells
2024-09-14
In addition to attracting immune cells to the site of injury, ROS also participate in proliferative responses during compensatory proliferation and regeneration. In Xenopus tadpoles, tail amputation induces sustained production of ROS over the span of regeneration, and decreasing ROS levels, especia
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br Materials and methods br Conflict of interest
2024-09-14
Materials and methods Conflict of interest Acknowledgments We thank Christine Heiner (Department of Surgery, University of Pittsburgh) for her critical reading of the manuscript. This work was supported by grants from the US National Institutes of Health (R01GM115366, R01CA160417, and R01CA
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br Introduction Alzheimer s disease AD is
2024-09-14
Introduction Alzheimer's disease (AD) is a neurodegenerative disorder and the leading cause of dementia. It is characterized by progressive and irreversible damage to different 20(S)-Hydroxycholesterol sale areas, resulting in cognitive impairment and behavioral changes (O'Neill, 2013, De Stroope
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br Materials and Methods br Results
2024-09-14
Materials and Methods Results Discussion Voluminous literature is available describing the regulation of Methylprednisolone homeostasis by central and peripheral mechanisms in poultry [35,36]. However, the neuroendocrine mechanism(s) of photoperiod induced hypothalamic regulation of food i
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FRAX486 We further analyzed selected hit compounds for their
2024-09-14
We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma FRAX486 were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin was employed as a
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Tacrine an aminoacridine derivative Fig
2024-09-14
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Finasteride has been shown to be a mechanism based
2024-09-13
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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