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Our overall goal is to
2022-01-14
Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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Herein we report the discovery of
2022-01-14
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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Lithocholic Acid The lactam compounds including ceftriaxone
2022-01-14
The β-lactam compounds, including ceftriaxone (CEF), have shown to attenuate drug-seeking in several drugs of abuse including methamphetamine [31], cocaine [32,33], nicotine [34] and morphine [35]. Moreover, in our laboratory, we have shown that CEF can reduce chronic alcohol drinking via upregulati
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br Conclusions br Acknowledgements br Introduction Glucose
2022-01-14
Conclusions Acknowledgements Introduction Glucose metabolism is vital to prepare uterine epithelium and stroma for embryo implantation and for the differentiation of the functionalis layer to support the developing conceptus [[1], [2], [3], [4]]. Due to its polar nature and hydrophilic cond
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Due to its unusually long pre implantation period the horse
2022-01-14
Due to its unusually long pre-implantation period [20,21], the horse conceptus is entirely dependent on histotrophic nutrition for the first 40 days of gestation [22]. During the pre-implantation period, glucose transporters in the endometrium and conceptus membranes must deliver the glucose require
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br Introduction The glucagon receptor GCGR
2022-01-14
Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m
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br Conflict of interest statement br
2022-01-14
Conflict of interest statement Acknowledgments Introduction Hedgehog (Hh) signaling controls key steps of development in most tissues and organs of invertebrates and vertebrates (Briscoe and Therond, 2013, Ingham et al., 2011, Wilson and Chuang, 2010). The unique cellular composition and mo
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The NVC response in the diseased or
2022-01-13
The NVC response in the diseased or aging Histamine Phosphate may be altered, including changes in both the chemical mediators of NVC, ion channel behaviour, and the dynamics of the vascular system. For example, in Alzheimer’s disease the production of NO is shown to be inhibited (Lourenço et al.,
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Introduction Histamine H Imidazol yl ethanamine mol w
2022-01-13
Introduction Histamine (2-(1H-Imidazol-4-yl)ethanamine), mol.w. 111.15 g/mol belongs to biogenic amines, which arise in foodstuffs from amino acids by action of microorganism´s or tissue enzymes. Histamine (HA) is formed from the amino W 54011 receptor L-histidine by action of enzyme histidine deca
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Work is presently underway to unveil mechanisms whereby
2022-01-13
Work is presently underway to unveil mechanisms whereby SAHA-dependent restoration of cardiomyocyte autophagic flux is protective. Another interesting question pertains to mechanisms whereby class I and class II HDAC inhibitors induce autophagy. It has been demonstrated that TSA reduces transverse a
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Biological evaluations of the compounds were
2022-01-13
Biological evaluations of the compounds were done both using HCV protease and replicon assays. Results are shown in . The protease inhibitory IC’s were determined using a FRET assay with HCV NS3/4A 1a protease domain. The replicon EC’s were determined using a replicon luciferase cell-based assay. Th
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Anhydrotetracycline hydrochloride synthesis Preliminary anal
2022-01-13
Preliminary analyses of these identified two bands for MALDI-TOF/TOF have shown the presence of approximately 20 proteins, most of which have not yet been characterized. However, several proteins, such as cytochrome c oxidase [53], peroxiredoin II E [54] and alcohol dehydrogenase [55], have been ide
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br Conflict of interest statement br Acknowledgments
2022-01-13
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg
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With the administration of OM
2022-01-13
With the administration of OM3 fatty acids, it has previously been shown that the activation of GPR120 is linked to the secretion and circulating levels of the adipokine adiponectin [123] promoting anti-inflammation (downregulation of NF-κB) and insulin sensitivity [124]. Interestingly, Nrf2 also de
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br Materials and methods br Results
2022-01-13
Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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