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Glucagon was described as an insulin
2021-09-23
Glucagon was described as an insulin secretagogue as early as 1965 (Samols et al., 1965). Our studies extend these findings by demonstrating that this is a direct effect mediated by distinct receptors in the mouse pancreas. Previous experiments on isolated β Nilvadipine mg clearly show that glucagon
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summarizes FAAH inhibition data for a
2021-09-22
summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibitio
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The present study was therefore conducted with
2021-09-22
The present study was therefore conducted with three aims; (1) we tested the effect of IRL-1620, a selective ETB receptor agonist, on the analgesic tolerance to morphine and oxycodone in mice; (2) we determined the expression of ETA receptors and ETB receptors in the Berbamine hydrochloride synthesi
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Evidence indicates that astrocytes play a role in the modula
2021-09-22
Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in
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The rationale for developing HDACi as anticancer agents
2021-09-22
The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Dutasteride arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematolog
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Since its development the HCV
2021-09-22
Since its development, the HCV replicon system (Lohmann et al., 1999) has been a critical tool in the HCV antiviral discovery process (Gottwein et al., 2009, Imhof and Simmonds, 2010, Lohmann et al., 1999, Pietschmann et al., 2001, Imhof and Simmonds, 2010, Gottwein et al., 2009). The replicon assay
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br sGC cGMP PKG pathway in
2021-09-22
sGC/cGMP/PKG pathway in regulation of platelet small GTPases All classical Rho family members of small GTPases including RhoA, Rac, Cdc42, some atypical Rho GTPases like RhoB, RhoF and RhoG, and also Ras family members N-Ras, K-Ras, Rap1A, Rap1B, Rap2A and Rap2B, and the Ras-related GTPases of th
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br Synthetic Antagonists for FFA To date only compounds
2021-09-22
Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this
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Ubiquitination of GlyRs subunit on
2021-09-22
Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor Ademetionine and subsequent degradation in lysosomes (Buttner et al., 2001). However, the specific E3 ligase responsible for GlyRs-α1 ubiquitination is largely unknown as yet. Also, the functional consequen
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To this end we evaluated novel
2021-09-22
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell perindopril erbumine systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6
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Cy5 amine (non-sulfonated) mg The dopamine substrate current
2021-09-22
The dopamine substrate currents (IDA – IControl) were determined at different holding potentials (IV curves) in transfected HT22 cells (Fig. 5A). The plot for HT22 cells transfected with DAT exhibited the typical behavior of dopamine transporter currents (Ingram et al., 2002; Sonders et al., 1997),
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Although it is mainly a glial protein of total
2021-09-22
Although it is mainly a glial protein, 5–10% of total GLT-1 represents a neuronal form located at presynaptic terminals, but its physiological role remains elusive (for discussion, see (Rimmele and Rosenberg, 2016)). Nevertheless, this amount might be significant since GLT-1 has been estimated to be
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br Conclusions We have shown that despite the development
2021-09-22
Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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Ac-IETD-pNA br Introduction The growth hormone secretagogue
2021-09-22
Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt
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There are additional implications of
2021-09-18
There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure
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