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Apatinib br Methods br Results br Discussion In this
2022-02-08
Methods Results Discussion In this study, we investigated temperature effects on Vj-gating properties of two cardiac GJs. In the case of Cx45 GJs, increased temperature from 22 °C to 28 °C (or 32 °C) led to an accelerated Vj-dependent deactivation with little change in the extent of Vj-gati
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In a follow up study the same
2022-02-08
In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c
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In the course of an internal FAAH program many
2022-02-08
In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on pr
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br Conclusion br Acknowledgements This work was
2022-02-08
Conclusion Acknowledgements This work was supported by R01 HL127386 (Niklason) and 1R01 HL128406-01A1 (Dardik), and by an unrestricted research gift from Humacyte Inc. KLL was supported by F30HL143880. KLL and EQ were supported by T32 GM007205. LEN is a founder and shareholder in Humacyte, Inc
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br Discussion This study dedicated to histamine H and H
2022-02-08
Discussion This study, dedicated to 33187 H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibition of transmitter r
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Treatment with histamine had no effect on histamine H
2022-02-08
Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 matrix metalloproteinases (Fig. 1), while knockdown of histamine H1 receptor expression prevented histamine from repressing apo A-I gene expression (Fig. 2). Overexpression of the histamine H1 receptor regulated apo
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The neurotransmitter histamine plays a
2022-02-08
The neurotransmitter histamine plays a key role in the sleep-wake cycle and in learning and memory. Alterations in KN-92 phosphate receptor histamine levels are closely connected with central nervous system dysfunction, and are thought to contribute to neurological disorders, including Alzheimer's d
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raas inhibitors G P also plays a critical role in regulating
2022-02-08
G6P also plays a critical role in regulating HK2 binding to mitochondria. Elevated levels of intracellular G6P weaken HK2 binding to mitochondria, causing the enzyme to translocate to the cytoplasm and facilitate anabolic glucose metabolism. Acidosis similarly induces HK2 translocation from mitochon
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The second class of proteins necessary
2022-02-08
The second class of proteins necessary for maintaining histamine-2 receptor antagonist dynamics is chromatin modifiers, which are considered ‘writers’ and ‘erasers’ and are responsible for modifications of histone N-terminal tails. These post-translational modifications can have direct or indirect e
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br Acknowledgments br Introduction Histone deacetylases HDAC
2022-02-08
Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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The relationship between increased GPR expression
2022-02-08
The relationship between increased GPR120 expression in the EDL skeletal muscle and systemic glucose control is yet to be investigated. However, if the increased expression of GPR120 correlates with enhanced insulin-stimulated glucose uptake in skeletal muscle, particularly the EDL muscle, this migh
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The pharmacokinetics of was obtained in mouse
2022-02-08
The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indicat
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SAR around amino derivative revealed a number of interesting
2022-02-07
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p
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br Acknowledgement The author expresses her
2022-02-07
Acknowledgement The author expresses her sincere appreciation to Brian P. Kenealy, Ph.D. for his contributions to the series of studies described in this article that were conducted during his tenure in the lab, as a graduate student first and then a postdoctoral research fellow. She also thanks
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In spite of the similarities
2022-02-07
In spite of the similarities of caffeine's effects in L929 cells and erythrocytes, a major difference can be identified in the magnitude of inhibition (35% versus 90%). It initially seems reasonable to conclude from this finding that the reduced magnitude of caffeine inhibition in L929 cells is simp
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