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br Conclusion Our data allow pharmacological discrimination
2022-09-17
Conclusion Our data allow pharmacological discrimination of diverse of H3 Tozasertib antagonists that can be linked to their differential efficacy in preclinical and clinical disease settings (Fig. 6). Moreover, we identify the sigma-1 receptor as a common “off target” for H3 antagonists, and tha
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Although we showed that RBL
2022-09-17
Although we showed that RBL-2H3 Sc98 ITE took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SERT for s
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br The hedgehog signalling pathway The
2022-09-17
The hedgehog signalling pathway The canonical Hh pathway is a conserved, highly complex signalling cascade, with many players and intricate regulation. However, it can be simplified into four fundamental components: i) the ligand Hh, ii) the receptor Patched (Patch [PTCH1]), iii) the signal trans
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br Gastrointestinal peptides and intestinal health Gastroint
2022-09-16
Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)
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br Introduction High dose niacin or nicotinic acid
2022-09-16
Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic Bromoenol lactone receptor form of niacin modulates plasma lipid profiles including d
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Adenosine Kinase Inhibitor hydrate mg TGR is a class A GPCR
2022-09-16
TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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br Conclusion br Introduction The
2022-09-16
Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri
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Pyrogallol is an organic gallic acid converting compound tha
2022-09-16
Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic Berberine hydrochloride receptor is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to p
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Ac-DEVD-pNA The potential therapeutic actions of GHSR in the
2022-09-16
The potential therapeutic actions of GHSR in the central nervous system has been in the limelight lately. Peripheral administration of GHSR agonists have been shown to inhibit oxidative stress, apoptosis, proinflammatory cytokine production, microglia activation, mitochondrial dysfunction, and excit
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Pyrimethamine Ghrelin is mostly known for its orexigenic pro
2022-09-16
Ghrelin is mostly known for its orexigenic properties, whereas the role of DAG on feeding is controversial with studies claiming an orexigenic, anorexigenic or no effect (Inhoff et al, 2009, Toshinai et al, 2006). One of these studies was that of Toshinai and colleagues, who found a link between the
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The first report about the activity of
2022-09-16
The first report about the activity of ANAM in CACs it is due to Garcia et al. [19] which treated 16 cancer patients with oral ANAM 50mg once daily vs placebo for 3days followed by a washout NHS-12-Biotin of 5–7days and then cross-over to the other group for 3 more days. It was described a weight g
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The importance of T currents
2022-09-15
The importance of T-currents in the control of thalamic GABA synaptic function is also demonstrated by the presence of T-channel-dependent long-term synaptic plasticity, either potentiation (LTP) or depression (LTD). Indeed, in the associative posterior thalamic medial nucleus, an LTP of the GABAerg
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The activation of GPR FFA signaling triggers the PLC PIP
2022-09-15
The activation of GPR40/FFA1 signaling triggers the PLC/PIP2 signaling pathway and results in Ca2+ release from the endoplasmic reticulum (ER). Increased Ca2+ levels may lead to activation of different protein kinases, such as Ca2+/calmodulin-dependent protein kinase type IV, Akt, extracellular sign
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These observations are of particular interest in the context
2022-09-15
These observations are of particular interest in the context of recent conceptual changes regarding the mechanisms by which different types of leukocytes contribute to atherogenesis. Over the last decade, the paradigm of the predominant circulatory origin of lesional macrophages has been challenged
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br Materials and methods br Results br Discussion In the
2022-09-15
Materials and methods Results Discussion In the absence of vascularization phenomena, endothelial cells (ECs) are among the most quiescent cells of the body [27]. ECs proliferation is significant during embryogenesis, as the vasculature is being formed, while in the adult life takes place o
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