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The third generation cephalosporin antibiotics can
2022-02-26
The third-generation cephalosporin α-mangostin can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when taken orally, CE
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While the apparent complexity of
2022-02-26
While the apparent complexity of gap junction regulation presents challenges, new technologies continue to propel the field forward. Advances in microscopy are increasingly able to capture rapid dynamics at the plasma membrane (e.g., biosensors [67] and lattice light sheet microscopy [100]) and to d
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br Secretase in inflammatory diseases
2022-02-26
γ-Secretase in inflammatory diseases γ-Secretase appears to play a more important role than previously recognized in inflammatory diseases. Studies have shown that mice partially deficient in PS genes (PS1+/− PS2−/−) develop an immune system deficit in late adulthood, such as ulcerated skin or a
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br The Farnesoid X receptor FXR
2022-02-26
The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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PBI is an agonist of GPR and
2022-02-26
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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depicts the synthesis of series with a four step
2022-02-26
depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (–)
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The precise mechanism by which erastin inhibits SLC
2022-02-26
The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A
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Therefore the histomorphology and the comprehensive analysis
2022-02-26
Therefore, the histomorphology and the comprehensive analysis of TMJ-RA pathogenesis need to be completed although clinical findings in TMJ-RA are similar to RA in other joints [41]. Especially for the dentist, the difficulties associated with diagnosing TMJ-RA patients [49] posing challenges to dia
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br Conclusions Symptoms from bilateral thalamic edema
2022-02-26
Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhibi
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Several observations about structure activity
2022-02-26
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic endothelin receptor antagonist class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replaci
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These agents can be divided into
2022-02-25
These agents can be divided into three categories based upon the therapeutic agent conjugated to the antibody; the most frequently explored are ADCs using a cytotoxic agent to be delivered directly to the tumor site. The second class has not been broadly used and consists of radionucleotides (Wong e
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ATP as a transmitter can be released
2022-02-25
ATP as a transmitter can be released from injured Eltrombopag and sensory nerve endings (Sperlágh et al., 1995, Sperlágh et al., 1997, Sperlágh et al., 1998, Burnstock, 2013, Burnstock, 2014). ATP can activate the P2X3 receptor in the DRG neurons (Gao et al., 2011a; Xu et al., 2012). In DRG neurons
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Zinc Pyrithione It is important to clarify
2022-02-25
It is important to clarify whether the decrease in USV after administration was secondary to the central depressant actions of the test compounds. Several reports have addressed the possibility that central depressant actions such as motor incoordination or changes in body temperature might affect U
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(R,S)-Anatabine For several parasites of veterinary importan
2022-02-25
For several parasites of veterinary importance, there is a growing body of evidence that resistance to ML is, at least in part, mediated by ABC transporters (P-glycoproteins) (Whittaker et al., 2017). P-glycoproteins (Pgps) are members of the ATP-binding cassette transporter family that are well kno
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Next we investigated the accumulation of H ribavirin
2022-02-25
Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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