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Based on our finding that TFA modulates
2021-10-13
Based on our finding that TFA modulates GlyR function and reports that TFA-bound Alrestatin can differ markedly from those synthesized without TFA, we retested a previously published dodecapeptide (D12-116) that also enhanced GlyR function but this time as a chloride salt (Tipps et al., 2010). No d
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Because AM had limited efficacy on rodent GPR
2021-10-13
Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to e
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In this study we present the synthesis and
2021-10-13
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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The transport of glutamate by EAAT from the
2021-10-13
The transport of glutamate by EAAT2 from the extracellular fluid into either astrocytes or endothelial cells is an unfavorable and energy-consuming process. This energy is provided by a coupled co-transport of three sodium ions, one proton, and one glutamate molecule in the counter-transport of one
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Neuropeptide Y 13-36 (porcine) br A myriad of receptors in W
2021-10-13
A myriad of receptors in WM To complicate the picture, WM glia express numerous non-glutamatergic neurotransmitter receptors, a fact that is often underappreciated when considering pathophysiology. When examined in isolated optic nerve, a central WM tract completely devoid of neuronal synapses, r
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Immunohistochemistry analysis shown ghrelin and GHSR
2021-10-13
Immunohistochemistry analysis shown ghrelin and GHSR-1a immunostaining was located in the epithelial cells of LY 255283 receptor and ducts throughout the lactation, strong immunoreactive cells were detected in L30, L60 and L120 stage. The distribution of ghrelin has been shown in many tissues, incl
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Emergent studies have recently shown that Sherpas living at
2021-10-13
Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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Galanin mediates its activity by binding to three G protein
2021-10-13
Galanin mediates its activity by binding to three G-protein coupled receptor subtypes (designated GAL1-GAL3). Since GAL3 mRNA is found mainly in regions of the mesolimbic dopamine system, such as the ventral tegmental area, dorsal raphe nucleus, LC, amygdala, hippocampus, thalamus, hypothalamus, NAc
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It is well known that TLR induced
2021-10-12
It is well known that TLR4-induced inflammation is associated with behavioural alterations including fever, hypolocomotion, altered appetite, anxiety and anhedonia (Dantzer, 2006, Dantzer et al., 2008). The current data demonstrate that while PF3845 potently attenuates TLR4-induced cytokines in the
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Arena Pharmaceutical introduced a biaryl sulfone
2021-10-12
Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Several studies have indicated that PLD
2021-10-12
Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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Other N substituted carboxamide oxy
2021-10-12
Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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We have shown previously that
2021-10-12
We have shown previously that activation of the TGFβ/Smad signaling pathway in keratinocytes regulates PIK-90 mg cytoskeleton organization via non-genomic and genomic mechanisms and that RhoB gene is a target of Smad proteins [12,13]. Although the role of RhoB in early non-genomic TGFβ-induced cell
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br Surrogate ligands for GPR Although
2021-10-12
Surrogate ligands for GPR35 Although identification of endogenously produced chemicals with agonist action at GPR35 is of considerable importance, the ligands described above are far from ideal to probe the roles of GPR35. Surrogate ligands are therefore required. Until recently, the key GPR35 ag
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Ubiquitination of GlyRs subunit on plasma membrane has
2021-10-12
Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor Cy5.5 carboxylic acid (non-sulfonated) and subsequent degradation in lysosomes (Buttner et al., 2001). However, the specific E3 ligase responsible for GlyRs-α1 ubiquitination is largely unknown as yet. Also
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