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The results of cell culture models were further
2023-12-02

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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Introduction hydroxytryptamine HT is found throughout
2023-12-01

Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary AZ191 (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current classification
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br Disclosure br Acknowledgement br Introduction CYP
2023-12-01

Disclosure Acknowledgement Introduction CYP17A1 is a multifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activities and is essential for the biosynthesis of steroidal BI-D1870 in male testes and adrenal glands. The 17α-hydroxylase activity of CYP17A1 is involved in the conversi
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Skeletal pain associated with bone fracture
2023-12-01

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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br Mechanisms of GPCR internalization Like for other types o
2023-12-01

Mechanisms of GPCR internalization Like for other types of receptors, prolonged agonist stimulation often leads to GPCR internalization, which can occur via different pathways ∗[2], [20], [21], [22], [23]. Of these pathways, clathrin-mediated TAME sale (CME) is the best characterized and arguably
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br Acknowledgments br Introduction Angiotensin
2023-12-01

Acknowledgments Introduction Angiotensin II (AngII) is among the most potent vasoactive substances produced in humans. Its effects are numerous, from vasoconstriction to control of fluid and electrolytes balances. Many of the physiological and pathological effects of AngII are mediated by the
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br Materials and methods br Results br Discussion The novel
2023-11-30

Materials and methods Results Discussion The novel and central finding of the current study is that endothelial 12/15-LO rather than the monocytic/macrophagic 12/15-LO has a critical role in hyperglycemia-induced leukocyte adhesion and retinal endothelial barrier dysfunction. The following
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Fatostatin A receptor br Conclusion br Conflicts of interest
2023-11-30

Conclusion Conflicts of interest Introduction Alzheimer’s disease is the most common neurodegenerative condition known to cause dementia (Ferri et al., 2005). Alzheimer’s dementia typically presents with initial recent episodic memory deficits, word finding difficulty and later with apraxia
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Interaction between AhR and ligands
2023-11-30

Interaction between AhR and ligands leads to AhR transformation (Fig. 1), characterized by a rapid receptor nuclear translocation and the formation of AhR/Arnt complex and the release of the chaperone proteins. Following AhR transformation, the AhR/Arnt complex binds to its cognate DNA consensus seq
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Introduction Epinephrine is an endocrine
2023-11-30

Introduction Epinephrine is an endocrine hormone mainly produced by adrenal medulla in response to stress (Tank and Lee Wong, 2015). This catecholamine exerts various major physiological effects, concerning notably the cardiovascular system, the respiratory system and the endocrine system, through
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The second evidence comes from the results obtained by patch
2023-11-30

The second evidence comes from the results obtained by patch-clamp recordings carried out at the endplate region of isolated mouse FDB fibers, where adenosine and the P1R agonist NECA significantly affected the NPo, the open frequency and the time constant τ of the adult nAChR channels. It is genera
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We also investigated the transmittance of actin polymerized
2023-11-30

We also investigated the transmittance of actin polymerized with and without ABP. The presence of actin in the solution results in an increment in turbidity as other proteins provided daunorubicin features [21], [32]. While G-actin showed a transmittance peak positioned at 241 nm, F-actin exhibited
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At the last follow up nine patients
2023-11-30

At the last follow-up, nine patients had discontinued pyridostigmine within the first year postoperatively. Only one patient required pyridostigmine at a higher dose, but this was accompanied by successful weaning of prednisolone. None of the 5 patients who were on pyridostigmine treatment alone pri
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The adult muscle type acetylcholine receptor AChR the
2023-11-30

The adult muscle-type Z-LEHD-FMK receptor (AChR), the exemplar pLGIC, is a heteropentamer comprising two α subunits, and one each of the β, δ, and ɛ subunits (Sine, 2012). These five subunits come together in a counterclockwise α-ɛ-α-δ-β arrangement (Figure 1A). Binding of acetylcholine to the AChR
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As mentioned above variation of the A ring was undertaken
2023-11-30

As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to Adenine (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comparable inhibi
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