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Histamine functions as a key neurotransmitter in multiple
2022-01-20

Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, Gap19 is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway (Bo
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Having shown that some of substitutions Cl CF at the
2022-01-20

Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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br Methods br Results br Discussion In
2022-01-20

Methods Results Discussion In this study, we investigated temperature effects on Vj-gating properties of two cardiac GJs. In the case of Cx45 GJs, increased temperature from 22 °C to 28 °C (or 32 °C) led to an accelerated Vj-dependent deactivation with little change in the extent of Vj-gati
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Cx mimetic peptides short synthetic peptides corresponding t
2022-01-20

Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino bromocriptine mesylate sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function
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AACOCF3 FPR family Human FPR was first defined biochemically
2022-01-20

FPR family Human FPR was first defined biochemically, in 1976, as a high affinity binding site on the surface of neutrophils for the prototypic N-formyl peptide formyl-methionine-leucyl-phenylalanine (fMLF). It was then cloned in 1990, by Boulay et al. from a differentiated HL-60 myeloid leukemia-c
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SC 560 mg Considering together the conformational docking an
2022-01-20

Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req
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br Acknowledgments This research was supported by the Nation
2022-01-20

Acknowledgments This research was supported by the National Institutes of Health Grants GM58442 and GM084152, as well as the National Institutes of Health Predoctoral Training Grant 5T32GM008700-13. We thank Eric Oldfield (University of Illinois, Urbana-Champaign) for providing the FDPS inhibitor
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Collectively these observations demonstrate that
2022-01-20

Collectively, these observations demonstrate that FAAH is functionally positioned to modulate the actions of AEA and other NAEs on BLA neurons and anxiety processes mediated by this region. By extension, manipulations that lead to alterations in FAAH activity, such as stress or administration of com
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RGFP966 Hexokinases HXKs are major regulatory enzymes in sug
2022-01-20

Hexokinases (HXKs) are major regulatory enzymes in sugar metabolism and in sugar sensing in plants (Claeyssen and Rivoal, 2007, Granot et al., 2013, Sheen, 2014, Aguilera-Alvarado and Sánchez-Nieto, 2017). HXK can phosphorylate both glucose and fructose to respective hexose-6-phosphates as a first s
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Among the isoforms of heme oxygenases HO HO and
2022-01-20

Among the 3 isoforms of heme oxygenases (HO-1, HO-2, and HO-3), HO-1 expression is inducible, and it catalyzes the degradation of heme to biliverdin, carbon monoxide (CO) and free Fe. The Fe is then stored in ferritin, limiting its ability to participate as a catalyst through the Fenton reaction and
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br Introduction Human immunodeficiency virus HIV is a retrov
2022-01-19

Introduction Human immunodeficiency virus-1 (HIV-1) is a retrovirus that primarily infects components of the human immune system, such as CD4+ T cells, macrophages and dendritic Amikacin disulfate (Clapham and McKnight, 2001). HIV directly and indirectly destroys CD4+ T cells, which leads to seve
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Finally we investigated increasing basicity as a
2022-01-19

Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, L-690,330 mg demonstrated significant improvement of values of solubility for the two media, especially f
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br Materials and methods br Results br Discussion Until very
2022-01-19

Materials and methods Results Discussion Until very recently, the anti-atherogenic activity of niacin was attributed almost exclusively to its impact on HDL and other plasma lipids, perhaps mediated via its action on GPR109A expressed in adipose or other tissues. However, recent clinical st
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On the other hand it is
2022-01-19

On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th
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br Experimental procedures br Results br Discussion Although
2022-01-19

Experimental procedures Results Discussion Although the presence and localization of the GlyR subunits have been determined in the adult retina, the proportion of each GlyR subunit has not been assessed in the adult or in the developing retina. In the present study, we carried out the absol
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