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The excitatory amino acid L glutamate or
2021-02-23

The excitatory amino Cyclo(RGDyK) L-glutamate or glutamate mediates most of the excitatory neurotransmission within the mammalian central nervous system (CNS) and has been implicated in numerous peripheral nervous system (PNS) pathways. The excitatory amino acids, including glutamate, are of great p
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α-Naphthoflavone Interestingly Carver Johnson and Kim
2021-02-23

Interestingly, Carver, Johnson, and Kim (2016) investigated a polymorphism in the OPRM1 μ-opioid receptor gene for its role in sensitivity to social contexts. The G allele of this polymorphism was associated with higher levels of sensitivity. The authors found significant interactions, e.g. the nega
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Given the potency enhancing effect of the butyl group
2021-02-23

Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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EC barrier dysfunction triggered by inflammatory mediators
2021-02-23

EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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PGE exerts its functions by binding to different receptors
2021-02-23

PGE2 exerts its functions by binding to different receptors. Four different subtypes of PGE2 receptors are found in mammals and are designated as EP1-4. These are G-protein coupled receptors that belong to a family of seven rhodopsin-like transmembrane spanning receptors. They are structurally diffe
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opioid receptors EP EP and EP receptor
2021-02-23

EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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Our research has demonstrated that the absolute bioavailabil
2021-02-23

Our research has demonstrated that the absolute bioavailability of oxymatrine, having a similar structure with OSC, was only 6.79±2.52%. About 50% of OSC was converted to its active metabolite SC in vivo; hence, the absolute bioavailability of OSC was speculated to be poor as well [24]. Understandin
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br Mass spectrometry based technologies Oxysterols tend not
2021-02-23

Mass spectrometry-based technologies Oxysterols tend not to be observed in global lipidomic analysis, whether shot-gun based electrospray ionisation – mass spectrometry (ESI-MS) or liquid chromatography (LC)-MS based. This is because of their comparatively low-abundance and poor ionisation charac
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The outcome of DGK function will thus
2021-02-23

The outcome of DGK function will thus depend on the binding partners of each DGK isoform, and the effects that they exert can be quite different. A clear example of this concept has been demonstrated for the type IV DGKs, ζ and ι, which are structurally very similar but have opposing effects on Ras
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Cysteinyl leukotrienes CysLTs are potent inflammatory mediat
2021-02-22

Cysteinyl leukotrienes (CysLTs) are potent inflammatory mediators closely associated with cerebral ischemic injury. CysLTs induce inflammatory responses mediated by at least two different CysLT receptors (CysLT1R and CysLT2R) (Bäck et al., 2011, Singh et al., 2010). It has been reported that the Cys
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Previous studies reported that NE and MHPG are deeply involv
2021-02-22

Previous studies reported that NE and MHPG are deeply involved in depression and that NE reuptake inhibitors are approved for use in patients with depression (for review, see [2]). We found increased hippocampal content of NE and MHPG in the CORT-treated CRTH2−/− mice (Fig. 3). In the hippocampus, a
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Propranolol initially discovered in is first and most widely
2021-02-22

Propranolol, initially discovered in 1964, is first and most widely studied as a non-selective beta-blocker. Propranolol through β-adrenergic receptor blockade has reduced heart rate and blood pressure and have anti-arrhythmogenic and anti-ischemic effects, and been proposed as an effective strategy
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Although it remains an unsettled issue evidence favors that
2021-02-22

Although it remains an unsettled issue, evidence favors that the endothelin ETA β-Tocotrienol receptor may play a more important pathological role. While both endothelin ETA and ETB receptors are found in most tissues, endothelin ETA receptor is the predominant receptor responsible for the vasoconst
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Recent pharmacological and clinical studies suggested that
2021-02-22

Recent pharmacological and clinical studies suggested that estetrol (E4) should also be considered as an interesting candidate for MHT (Abot et al., 2014; Mawet et al., 2015). E4 is naturally produced from E2 and estriol (E3) via 15α- and 16α-hydroxylase by the human fetal liver during pregnancy and
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Recent studies have shown that the extracellular regulated p
2021-02-22

Recent studies have shown that the extracellular regulated protein kinase 1 and 2 (ERK1 and ERK2), commonly referred to collectively as ERK 1/2, are members of the mitogen-activated protein kinase (MAPK) family. This family of kinases transport signals from the surface of the cell to the nucleus, th
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