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Another interesting approach is to
2022-03-16

Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain
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We have shown previously that activation of the
2022-03-16

We have shown previously that activation of the TGFβ/Smad signaling pathway in keratinocytes regulates LED209 cytoskeleton organization via non-genomic and genomic mechanisms and that RhoB gene is a target of Smad proteins [12,13]. Although the role of RhoB in early non-genomic TGFβ-induced cell re
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In the present study we showed that
2022-03-16

In the present study, we showed that reduced neuron formation in vitro induced by IL-1β was ameliorated by activation of GPR55 in both human and mouse cultures of NSCs. Pre-treatment with GPR55 agonists also blocked upregulation of inflammatory cytokine receptor mRNA (IL-1R1, IL-6st) while increasin
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br Niacin has long been used for
2022-03-16

Niacin () () has long been used for the treatment of lipid disorders and for the prevention of cardiovascular disease, the leading cause of death in the U.S., as a result of its ability to raise high-density lipoprotein (HDL) levels. Recent mechanistic investigations have shown that niacin may exe
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This evidence suggests that the human cochlea
2022-03-16

This evidence suggests that the human cochlea is equipped with antigen presenting macrophages as well as T lymphocytes that execute cytotoxic and immune mediation function. In an animal study, following acoustic overstimulation, Yang et al. (2015) found infiltration of macrophages into the region of
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Growing evidence suggests that the glycine
2022-03-16

Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it donepezil hydrochloride has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). Mo
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To this end we evaluated novel D analogs for selectivity
2022-03-16

To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell atipamezole systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-substitu
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The dopamine substrate currents IDA
2022-03-16

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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br Introduction Glucokinase GCK hexokinase IV is a monomeric
2022-03-16

Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter i
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Whether or not SMO and SMO dependent HH signaling
2022-03-16

Whether or not SMO and SMO-dependent HH signaling play a role in hematopoiesis is a subject of strong controversy. Obviously, the effects of SMO deletion are highly contextual and dependent on the timing of deletion. transplanted murine Smo−/− fetal liver L-745,870 trihydrochloride into sublethall
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Recently several dual GLP GIP receptor agonists have
2022-03-16

Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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Isolation and application of cold adapted
2022-03-16

Isolation and application of cold-adapted β-galactosidase in the production of low lactose dairy products would play a critical role in improving access to low lactose dairy products for lactose intolerant individuals [9,11]. Milk contains high levels of K+, Ca2+, and Na+, and β-galactosidase used i
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We tested formyl MYVKWPWYVWL which we had previously
2022-03-16

We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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br Acknowledgments R Dalmann has obtained a bourse Cifre gra
2022-03-15

Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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Methods br Results br Discussion SV exocytosis from excitato
2022-03-15

Methods Results Discussion SV exocytosis from excitatory boutons is more sensitive to inhibition by isoflurane than exocytosis from inhibitory boutons,4, 31 but the mechanism(s) of this synaptic selectivity is unknown. Although P/Q-type VGCCs contributed quantitatively more to SV exocytosis t
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