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Neuropathic pain NP is a chronic pain caused
2021-11-02
Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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Epigenetic inheritance is regarded as the genetic
2021-11-02
Epigenetic inheritance is regarded as the genetic modification of Cholic acid mg that affects gene expression and related processes of other DNAs but does not directly change the DNA coding sequence [18]. Epigenetic inheritance includes DNA methylation, histone modification, and noncoding RNA expre
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We thus asked whether enhanced AEA levels
2021-11-01
We thus asked whether enhanced AEA levels in the Efavirenz reduce the level of age-related inflammatory changes and slow down brain ageing. To answer this question we compared the morphology of microglia and level of pro-inflammatory cytokines in the hippocampus of young and old wild-type and FAAH−
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br Hippo pathway signalling The
2021-11-01
Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular Sulbactam status [10]. This pathway is linked to development, cell proliferati
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Silydianin br Membrane Fusion Requires Rab GTPases Tethers a
2021-11-01
Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e
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After establishing improved GSNOR potency some of
2021-11-01
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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The rat model was validated with another agonist of
2021-11-01
The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L
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Hypertriglyceridemia is associated with an overproduction an
2021-11-01
Hypertriglyceridemia is associated with an overproduction and secretion of triglyceride-rich lipoproteins (TRLs), due to increased liver lipid substrate availability (Adiels et al., 2005, Choi and Ginsberg, 2011), and/or reduced catabolism of TRLs and their remnants, due to reduced lipoprotein lipas
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Much of the understanding of this system has
2021-10-29
Much of the understanding of this system has come from several studies focussed on CB1. A significant amount of research has demonstrated that activation of the CB1 receptor by cannabinoid ligands stimulates food intake [10], reduces gastrointestinal motility [11], and increases lipogenesis [12] and
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The atherosclerosis development requires additional pro infl
2021-10-29
The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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br Synthetic Antagonists for FFA To date only
2021-10-29
Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this
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Because of the commercial availability of some acetamide
2021-10-29
Because of the commercial availability of some acetamide phenol starting materials, a few acetamide final products (such as and , ) were directly synthesized via a Mitsunobu reaction with chloropyrimidine piperidinyl cyclopropyl alcohol . The 3-pyridinyl analogue was synthesized by a nucleophilic
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GPR is a member of the G protein coupled
2021-10-29
GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c
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The neuronal glycine receptor HSOR allopregnanolone pathway
2021-10-29
The neuronal glycine receptor/3α-HSOR/allopregnanolone pathway may also be extended to the central nervous effects of gelsemine and koumine in brain. 3α-HSOR is expressed in certain brain regions in rats and humans, such as the limbic system including hypothalamus, hippocampus and amygdala, in addit
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HBX 41108 The main results whose proofs depend on the explic
2021-10-29
The main results, whose proofs depend on the explicit calculation of , include To set our work into the historical context, we note that the transporter category algebras are skew group algebras, and thus are fully group-graded algebras. This work is partially motivated by the papers on fully group
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