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A more refined picture of cholinesterase
2020-09-11
A more refined picture of cholinesterase activity patterns may be obtained by measuring ChE activity of the same sample before and after addition of certain cholinesterase inhibitors, with differential specificity for different components of total ChE activity, such as BW284c51 (BW1,5-bis-(4-allyldi
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br Introduction The cys loop ligand gated ion channels LGICs
2020-09-11
Introduction The cys-loop ligand gated ion channels (LGICs) are membrane-bound proteins mediating fast transduction from chemical to electrical signals at neuronal synapses and neuromuscular junctions [1], [2]. Each subunit that makes up the pentameric LGIC architecture possesses a dicysteine bri
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Cell swelling stimulates the release of certain amino
2020-09-11
Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino methylergometrine synthesis taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that
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br Experimental Procedures br Author Contributions br Acknow
2020-09-11
Experimental Procedures Author Contributions Acknowledgments Introduction Estrogen-related receptors (ERRα, ERRβ, and ERRγ) are orphan nuclear receptors whose physiological ligands have not yet been identified. Although ERRs are closely related to estrogen receptors (ERs) they do not res
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In addition to the ESIs identified that target both EPAC
2020-09-11
In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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In addition PK studies on indicate that it displays
2020-09-11
In addition, PK studies on indicate that it displays excellent bioavailability, pharmacological and toxicological parameters., A concern was initially raised about compound that it may cause EPAC denaturing properties and false positives. To address this issue, Cheng and co-workers have conducted
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Previously we have reported that magnitude
2020-09-11
Previously, we have reported that magnitude of the disruption of the blood–aqueous barrier after paracentesis was reduced by 82% in EP4 receptor knockout mice (Biswas et al., 2006). In the present study, we observed that pretreatment of EP1 receptor knockout mice with EP4 receptor antagonist, reduce
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EP EP and EP receptor expression
2020-09-11
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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Repulsive interactions towards undesirable substrates are ar
2020-09-11
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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br Introduction In addition to the
2020-09-10
Introduction In addition to the canonical double stranded structure, DNA can form various higher order structures such as bulges, and various kinds of mismatches, triplexes, to the G-quadruplex (G4). Over the past decades, accumulating evidence has begun to emerge that these non-canonical structu
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br Results and discussion To check the
2020-09-10
Results and discussion To check the punicalagin that the charge of α-synuclein can be altered due to the glycation, we measured zeta potential of native α-synuclein and α-synuclein glycated by two different glycating agents, methylglyoxal (MG) and glyceraldehyde-3-phosphate (GA-3-P). The value f
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As the COMT enzyme is primarily
2020-09-10
As the COMT enzyme is primarily related to prefrontal dopamine degradation (e.g., Yavich et al., 2007), the present study supports the notion that prefrontal dopamine modulates retention of fear extinction rather than within-session extinction (Abraham et al., 2014). Consistent with other studies we
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In the particular case of
2020-09-10
In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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It is now known that cholinergic signaling
2020-09-10
It is now known that cholinergic signaling plays a vital role in controlling many peripheral functions including skeletal and smooth muscle contraction, autonomic postganglionic neuron activation, parasympathetic end-organ activation (e.g., salivary, lacrimal and bronchial glands), regulation of car
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The major concern of PDE
2020-09-10
The major concern of PDE-5-I use in liver cirrhosis is the potentially harmful effect on systemic blood pressure. Data of clinical studies are conflicting [27], [30], [31], [32], but available patient details suggest that in advanced liver cirrhosis, PDE-5-Is lower systemic blood pressure to a great
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