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Receptor guanylyl cyclases play essential roles
2022-04-07
Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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Compared with the tetrazole derivative the potency of analog
2022-04-06
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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Routine administration of exogenous GC is pertinent
2022-04-06
Routine administration of exogenous GC is pertinent during late gestation, particularly in women who are at risk of delivering a preterm infant, aiming at ensuring proper neonatal outcome and survival (Kamath-Rayne et al., 2012). Unfortunately, despite its beneficial roles in foetal survival, variou
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In the pathogenesis of insulin resistance
2022-04-06
In the pathogenesis of insulin resistance, chronic activation of inflammatory pathways plays an important role, and the macrophage/adipocyte inter-communication provides a key mechanism underlying the common disease states of decreased insulin sensitivity [10]. This involves the migration of macroph
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GPR is a member of the
2022-04-06
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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Retapamulin Previously we have shown that rapid action
2022-04-06
Previously, we have shown that rapid action of E2in vitro is mediated through two E2 membrane receptors, GPR30 (GPER1) and the STX-sensitive membrane receptors (Noel et al., 2008; Kenealy et al., 2011a, Kenealy et al., 2011b). This is significantly different from receptors implicated in the positive
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Z VDVAD FMK The amyloid precursor protein APP is a membrane
2022-04-06
The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s
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br Introduction The generic antifibrinolytic drug tranexamic
2022-04-06
Introduction The generic antifibrinolytic drug tranexamic Edrophonium chloride mg (TXA) inhibits the protein-protein interaction between plasminogen and fibrin [9]. TXA is frequently used to reduce bleeding in various hemorrhagic conditions, such as during surgical procedures in the heart [19].
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ICH induced striatal lesion produced a reduction
2022-04-06
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino GSK2636771 transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia
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In spite of the similarities of caffeine s effects in
2022-04-06
In spite of the similarities of caffeine's effects in L929 cells and erythrocytes, a major difference can be identified in the magnitude of inhibition (35% versus 90%). It initially seems reasonable to conclude from this finding that the reduced magnitude of caffeine inhibition in L929 cells is simp
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The experiments indicate that a major component of the
2022-04-06
The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in adenylate cyclase preconstricted with α1-adrenoceptor agonists, phenylephrine or methoxamine, but not in ves
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br Structures of human secretase Before the near atomic reso
2022-04-06
Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a brucine chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were specul
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Galanin a amino acid peptide was
2022-04-06
Galanin, a 29/30-amino-acid peptide, was first isolated in 1983 from porcine intestine by Tatemoto and collaborators [70]. It is widely distributed throughout the central and peripheral nervous systems as well as other tissues. It is involved in a wide range of physiological functions, such as modul
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Target regulated the formation of G quadruplex was used here
2022-04-06
Target-regulated the formation of G-quadruplex was used here to “kill two ak7 with one stone” for the detection of melamine and I− with one probe DNA. G-quadruplexes are higher-order structures formed from G-rich oligonucleotides through the stacking of planar G-tetrads [43,44]. They have been exte
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To understand the impact of alterations in brain zinc homeos
2022-04-06
To understand the impact of alterations in Phosphoramidon Disodium Salt australia zinc homeostasis, the role of Zn2+ as a neurotransmitter has to be appreciated. Certain regions of the brain including the neocortex and hippocampus harbour so-called “zincergic” (or “gluzinergic”) neurons, where Zn2+
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