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Considering the fact that NADPH oxidase is the main source
2022-08-02

Considering the fact that NADPH oxidase is the main source for paraquat and maneb-induced oxidative stress, we hypothesized that NADPH oxidase activation might contribute to dopaminergic neurodegeneration induced by paraquat and maneb through ferroptosis. To test our hypothesis, we investigated the
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The exact mechanism by which N BPs
2022-08-02

The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs
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In summary we have discovered the first examples of movement
2022-08-02

In summary, we have discovered the first examples of movement of Asp189 upon binding to fXa inhibitors. A series of novel and potent fXa inhibitors with a phenyltriazolinone P moiety were identified. Although the general binding mode compared to our previously-reported fXa inhibitors was maintained,
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Saxagliptin br Characterization of quantal exocytosis by amp
2022-08-02

Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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Conflicting data concerning the involvement of H R
2022-08-01

Conflicting data concerning the involvement of H2R on glycaemia has also arisen. Its antagonism was reported to decrease [35], not affect [36], [37] and increase [38], [39] LY2940680 levels. In comparison, the clinical experience with antipsychotic drugs generated clearer evidence for the involvemen
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br Introduction Chronic hepatitis C CHC caused
2022-07-30

Introduction Chronic hepatitis C (CHC) caused by hepatitis C virus (HCV) infection affects approximately 170 million individuals worldwide [1]. HCV and human immunodeficiency virus (HIV) have similar routes of transmission, including blood-to-blood contact, sharing of injection equipment, and sex
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The relaxant response to carperitide was
2022-07-30

The relaxant response to carperitide was influenced neither by the removal of the endothelium nor by treatment with the nitric oxide synthase inhibitor or nitric oxide scavenger. This result was to be expected as previous studies showing that the vasodilator action of atrial natriuretic peptide is e
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In contrast the sGC activator
2022-07-30

In contrast, the sGC activator BAY 58-2667 relaxed the CC in a concentration-dependent manner (Figure 4B), a response that was significantly increased in the CC of sGCβ1ki/ki mice compared with WT mice. The finding that BAY 58-2667 also possessed a corporal relaxing effect in WT mice is suggestive b
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Bupivacaine is one of the local
2022-07-30

Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root HG-9-91-01 (DRG) neurons [5], [6], [
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br Materials and methods br Results br
2022-07-30

Materials and methods Results Discussion In this report, we have analyzed the function of an orphan GPCR, and GPR84, using genetically-deficient mice. The expression of GPR84 in the T and SB 203580 in the spleen prompted us to examine the functional responses of these cells under in vitro
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regadenoson Recently the novel fatty acid receptor GPR
2022-07-29

Recently, the novel fatty regadenoson receptor, GPR120 (also called FFAR4), has been shown to be implicated in diverse physiological homeostasis, such as insulin sensitization, anti-inflammation and regulation of appetite (Hirasawa et al., 2005, Oh et al., 2010). Notably, it is abundantly expressed
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The spatial effects of Ebi involve the
2022-07-29

The spatial effects of Ebi2 involve the creation of a moderate bias in CD4+ T cell distribution toward the LN periphery. Is this modest effect meaningful in an evolutionary sense? In this regard, we think the following considerations are relevant. First, asymmetric CD4+ T cell positioning is highly
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br Discussion Naloxone and CTAP were able to alter the
2022-07-29

Discussion Naloxone and CTAP were able to alter the febrile response induced by gp120. This effect was particularly evident during the initial hours following gp120 administration (90–210min). We also investigated the potential role of the delta-2 opioid receptor in gp120-induced fever. The delta
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In this study we present
2022-07-29

In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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Herein in consider of the
2022-07-29

Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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