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br ABCA is a sterol
2024-08-02
ABCA2 is a sterol-responsive gene The first evidence to demonstrate that ABCA2 expression responded to sterol loading was provided in an experiment involving monocyte to macrophage differentiation in vitro. Upon sterol loading with enzymatically degraded LDL (eLDL), ABCA2 expression increased onl
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Another open question is whether
2024-08-02
Another open question is whether GABA and ACh are released from the same synaptic vesicles, or even the same presynaptic terminals. Multi-transmitter neurons may either function through co-release, in which multiple neurotransmitters are packaged into the same presynaptic terminal and are therefore
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Anti LT therapy by LO inhibition has been
2024-08-02
Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [
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br Introduction Stroke is a devastating condition that cause
2024-08-02
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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Thymoquinone TQ is the major active
2024-08-01
Thymoquinone (TQ) is the major active Cytochalasin J australia derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005,
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raas inhibitor Earlier studies with SERMs identified that di
2024-08-01
Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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Thus far a tight coupling has been observed between
2024-08-01
Thus far, a tight coupling has been observed between mAbs that target aggregated Aβ and the occurrence of ARIA. If ARIA-E is caused by increased trafficking to and clearance of fibrillar Aβ from cerebral vessels (20), mAbs could be designed with conformationally specific epitopes selective for solub
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The observation that vortioxetine blocks HT induced currents
2024-08-01
The observation that vortioxetine blocks 5-HT-induced currents in 5-HT3 receptor-expressing oocytes suggests that vortioxetine acts to functionally antagonize these receptors, and is in line with previously published data (Bang-Andersen et al., 2011). For example, Mørk et al. (2012) demonstrated tha
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The nAChR has been considered an interesting potential targe
2024-08-01
The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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The present in vitro pharmacological experiments revealed th
2024-08-01
The present in vitro pharmacological experiments revealed that the cholinergic up-regulation of VEGF expression in neurons and astrocytes was mainly mediated by nicotinic AChR and muscarinic AChR, respectively. In addition, neuronal VEGF expression was elevated by endogenous ACh in a manner that was
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Finasteride was the first steroidal reductase
2024-07-31
Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH
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Phospholipases cleave membrane phospholipids from
2024-07-31
Phospholipases cleave membrane phospholipids from inflammatory cells, activated platelets, erythrocytes, adipocytes and cancer IAA-94 (Aoki et al., 2008, Neidlinger et al., 2006). Several reports have analysed the role of LPA and its receptors in the pathogenesis of RA. Zhao et al. reported that L
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br Introduction Cadmium is a major component of heavy metal
2024-07-31
Introduction Cadmium is a major component of heavy metal pollution. Phytoremediation is considered to be the more effective method for recovering contaminated soil [[1], [2], [3], [4]] via cadmium absorption, transport, and accumulation. Several cadmium-associated proteins have previously been we
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Neuropathic animals display increased sensitivity to
2024-07-31
Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB Phosphatase Inhibitor Cocktail 2 (100X in ddH2O) in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2
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Recent progress has been made in
2024-07-31
Recent progress has been made in translating animal findings on memory performance and amnestic effects – that are largely determined by tonically active receptors in which α5 contributes to the benzodiazepine binding site. Based on the observation that deletion of this subunit led to improved spati
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