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As part of their ongoing
2022-09-20
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile 550 24 synthesis derivatives
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GPR can signal through not only IP but also
2022-09-19
GPR40 can signal through not only IP3 but also cAMP depending upon the type of agonist ligand used. A full agonist engages both signaling mechanisms in contrast to the endogenous long-chain fatty SAR 405 (LCFA) ligands and partial agonists. Thus, stimulation of GPR40 by endogenous LCFAs or by the s
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Besides the described effects on gross locomotor function im
2022-09-17
Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t
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risedronic acid Data were collected using a Powerlab and Cha
2022-09-17
Data were collected using a Powerlab and Chart 5 software (ADInstruments, Bella Vista, NSW, Australia) and were analysed using GraphPad Prism 5 (GraphPad Software, San Diego, CA). Responses to ghrelin receptor agonists in phenylephrine, methoxamine, endothelin-1, U46619 and 60mM [K+] contracted vess
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Serotonin hydroxytryptamine HT is a monoamine
2022-09-17
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the Acridine Orange hydrochloride as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; D
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Hydantoin in region F bridging the phenoxybenzene and
2022-09-17
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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To explain the corporate debt maturity following Brockman et
2022-09-17
To explain the corporate debt maturity, following Brockman et al. (2010), the time-varying control variables we include are: firm size (LSIZE), the square of firm size (LSIZE2), leverage (LEVERAGE), asset maturity (ASSET_MAT), managerial ownership (OWN), market-to-book ratio (MB), term structure of
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FXa is a vitamin K
2022-09-17
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Reversine sale and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The
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The organ culture method has previously shown to be
2022-09-17
The organ culture method has previously shown to be a suitable model for investigations of receptor upregulation on vascular smooth muscle cells (Adner et al., 1996). In our study, the organ culture method was applied in order to examine whether LPS from P.g. was capable of altering the gene express
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In the CNS histamine is known to regulate sleep and
2022-09-17
In the CNS, S/GSK1349572 is known to regulate sleep and wakefulness, learning and memory, feeding, and energy. Here, we address its actions in relation to CNS disorders, and emphasize potential clinical applications of histamine receptor ligands (Table 1). In addition, as the effect of histamine on
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There were limitations to this study Specifically although r
2022-09-17
There were limitations to this study. Specifically, although rigorously examined for accuracy, the NCDB and SEER databases still suffer from issues with data entry and completeness of the treatment record. Of note, although the data were collected on a modern cohort of patients treated from 2010 to
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Ac-IETD-pNA Based on the in vitro findings summarized
2022-09-17
Based on the in vitro findings summarized here, we posited that, in the intact brain, release of ROS from iron-laden astrocytes to the local neuropil elicits oxidative damage and degeneration of indigent dopaminergic projections and other vulnerable neuronal elements (Schipper, 2001). Of particular
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The importance of FXR FGF signaling in BA homeostasis
2022-09-16
The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P
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In response to oxidative stress in DM antioxidant
2022-09-16
In response to oxidative stress in DM, antioxidant defence systems are activated in β-cells. Glutathione (GSH) is one of the most abundant antioxidants and has been shown to be expressed at lower concentrations in patients with DM [12], [13]. Furthermore, plasma levels of glycine, which is a synthet
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Although we showed that RBL H
2022-09-16
Although we showed that RBL-2H3 Sc98 CORM-3 took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SERT fo
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