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br Ethics approval br Availability of data and
2022-08-13
Ethics approval Availability of data and materials Consent for publication Competing interests Authors contributions Introduction Glucose supply to tissues is maintained through a complex regulatory network mostly driven by the pancreatic hormones insulin and glucagon which control
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Since we were able to reach low
2022-08-13
Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr
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In the present studies we found that genistein did not
2022-08-13
In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 6 ohda sale and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS) production i
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Herein we report the discovery of
2022-08-13
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Treatment with histamine had no
2022-08-13
Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 M871 (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 A-I promoter activit
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The Hardy Weinberg equilibrium was verified in
2022-08-12
The Hardy-Weinberg equilibrium was verified in all groups using the chi-square test. Using WINPEPI 11.65, the number of carriers and non-carriers of the Δ32 allele was compared between the groups through the Pearson's chi-square test with Yates's correction. Two-tailed Fisher's test was used when ap
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Alzheimer s disease AD is a neurodegenerative
2022-08-12
Alzheimer's disease (AD) is a neurodegenerative disorder and characterized by the presence of abnormal filamentous protein inclusions in nerve cells of the brain [2]. The neuropathological hallmarks of AD were first reported by Alois Alzheimer and date back to 1907 [3], [4]. These inclusions are fo
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br Methods and materials br Acknowledgements
2022-08-12
Methods and materials Acknowledgements The authors thank the NIH AIDS Reagent Program for providing the materials and reagents. The HIV-1 1084i envelope gene was a generous gift from Dr. Charles Wood. This work was supported in part by grants to S.-H. X. from the Bill and Melinda Gates Foundat
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The dramatic increase in the development of EAAT inhibitors
2022-08-12
The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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Ironically another series of studies examining the role of E
2022-08-12
Ironically, another series of studies examining the role of EAATs in CNS injury and disease suggest that under some pathological conditions, the operation of the EAATs is not protective, but actually contributes to the excitotoxic process (Rossi et al., 2000). The transporters do so by serving as th
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Results indicated that superfusion of orexin alone glutamate
2022-08-12
Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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To assess whether this coupling mechanisms might operate als
2022-08-12
To assess whether this coupling mechanisms might operate also in a native system of untransfected cells, we select a cell line SH-SY5Y neuroblastoma that is known to express both the dopamine transporter and the M-currents (Jiang et al., 2004; Wickenden et al., 2008). These experiments were performe
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In the present study we
2022-08-12
In the present study, we tested α-glucosidase and tyrosinase inhibitory effects of the methanol extract from lower stems and hippo pathway of Q. coccifera (1) as well as the isolated compounds [lyoniresinol-9-O-β-xylopyranoside (2) and lyoniresinol-9-O-β-glucopyranoside (3), cocciferoside (4), (-)-
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While ghrelin s role in addictive behaviors has been most
2022-08-12
While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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br Conclusion In the present study we
2022-08-12
Conclusion In the present study, we found that the majority of commercially available antibodies and antibody-based tools against galanin and its receptors that we tested do not meet validation requirements. Therefore, critical validation of these tools by the user is essential before being used
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