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As comparators compounds and were made
2022-08-12

As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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The physiological role of lactate induced
2022-08-12

The physiological role of lactate-induced antilipolytic effects is less clear. It has been speculated that GPR81 mediates the inhibition of lipolysis during intensive exercise, a condition which results in high systemic lactate plasma concentrations 9, 10. Owing to oxygen shortage resulting from int
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The amyloid precursor protein APP is a membrane
2022-08-12

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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Several groups studied CTD mouse
2022-08-12

Several groups studied CTD mouse models, which largely mimicked the symptoms (i.e. impaired cognition and autistic-like behaviour) of the human disease (Kurosawa et al., 2012; Baroncelli et al., 2016; Stockebrand, 2018). The CRT-1 knockout mice showed a drastic deterioration in the GABAergic system,
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Analysis of genomic neighborhoods has helped resolve questio
2022-08-12

Analysis of genomic neighborhoods has helped resolve questions concerning the orthology of receptors for peptides similar to glucagon (Ng et al., 2010, Irwin and Prentice, 2011, Wang et al., 2012, Hwang et al., 2013). Using a diverse array of species with available genome sequence (see Fig. 4) the g
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alzheimer's disease Regulation of pancreatic and cell ma
2022-08-12

Regulation of pancreatic α and β cell mass has been extensively studied and hotly debated, due to potential therapeutic implications. Early claims of Angptl8 as “betatrophin” and Angptl4 as a regulator of glucagon secretion and α cell proliferation (Yi et al., 2013, Ben-Zvi et al., 2015) have not st
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Genetic contributions to this dysregulation of expression ha
2022-08-11

Genetic contributions to this dysregulation of expression have been studied, and significant associations have been found. The Fas −670 polymorphism is associated with preterm premature rupture of membranes, preeclampsia, as well as intrauterine growth restriction [7], [16]. The Fas SNP (−670 A>G) i
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Neuropathic pain NP is a chronic pain caused
2022-08-11

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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SU 4312 receptor br Conclusion We have demonstrated
2022-08-11

Conclusion We have demonstrated that ETB receptors negatively regulate the expression of AT1 receptors in renal proximal tubule SU 4312 receptor from WKY rats but not in SHRs. Short-term activation of the ETB receptor increases AT1 receptor phosphorylation in WKY cells but decreases it in SHR ce
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TUG 891 br Materials and methods br
2022-08-11

Materials and methods Results Discussion Although there is general agreement that GPR109A has anti-lipolytic activity and that the NEFA reduction in response to nicotinic TUG 891 is mediated by GPR109A, whether GPR109A activation has any impact on plasma TG levels is unclear. Since the phen
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br Materials and methods br Results
2022-08-11

Materials and methods Results Discussion Main results obtained in this work are presented in Table 1 and can be summarized as follows: 1) AEA inhibits FcεRI receptor-induced degranulation with the participation of CB2 and GPR55 receptors by a PTX-insensitive mechanism; 2) AEA does not block
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In addition researchers studying GPR
2022-08-11

In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it TMC647055 Choline salt receptor is unclear why Sanofi-Aventis chose to terminate collabo
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Our data for glucose and insulin
2022-08-11

Our data for glucose and insulin tolerance tests indicate that niacin-induced hyperglycemia is proportional to the degree of insulin resistance induced, implying that there is deterioration in islet function with niacin treatment (McCulloch et al., 1991). In this regard, we have demonstrated, for th
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br Results and discussion br Conclusion In conclusion
2022-08-10

Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios
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The primary requirements of an ideal bioprobe for
2022-08-10

The primary requirements of an ideal bioprobe for glucose transporter-mediated bioimaging include high specificity, sensitivity as well as low cytotoxicity [18]. According to these concepts, we recently reported the simple amide linked glycoconjugates which containing cyanine fluorophores (Cy3 and C
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