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As comparators compounds and were
2022-01-14
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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Recently an increasing number of
2022-01-14
Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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br Potential endogenous agonists of GPR The
2022-01-14
Potential endogenous agonists of GPR35 The first endogenously produced chemical that was shown to be able to activate GPR35 was the tryptophan metabolite kynurenic lactacystin [8]. When human GPR35 was expressed along with a mixture of promiscuous and chimeric G proteins 9, 10 (Box 1) in CHO cel
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br Materials and methods br Results br Discussion br Disclos
2022-01-14
Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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The timing and growth of follicles relative to follicle devi
2022-01-14
The timing and growth of follicles relative to follicle deviation was assessed in 49 cows (Fig. 4) that had NFWE following treatment onset and that had not already established dominance. Because day of deviation did not differ due to treatment, day of estrous cycle, or replicate, data are presented
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Rapid action of E on GnRH neurons
2022-01-14
Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor
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br Materials and methods br Results br Conclusions We develo
2022-01-14
Materials and methods Results Conclusions We developed a glutamate biosensor with chitosan as a matrix for the immobilization of the enzyme glutamate oxidase on the surface of a platinum electrode. Our miniaturized biosensor of 50 µm in diameter can be applied for monitoring glutamate in vi
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br Secretase modulators a loss of pharmacology A
2022-01-13
γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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Development of few more dihydroxy
2022-01-13
Development of few more dihydroxy-pyrimidine and N-methylpyrimidone analogues as HIV-integrase inhibitors was attempted involving substitution of variety of five- and six-membered rings via the introduction of a simple methyl substituent in the α-position of the C-2 side chains in order to improve p
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Some studies using RNAi have recently been invalidated
2022-01-13
Some studies using RNAi have recently been invalidated by CRISPR/Cas9 [25] due to significant off-target effects of RNAi [26]. In this study, we have used both RNAi and CRISPR/Cas9 techniques and have observed consistent and similar phenotypes thus; knockdown or knockout of PATZ1 resulted in reducti
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The neurotransmitter histamine plays a key role in the
2022-01-13
The neurotransmitter histamine plays a key role in the sleep-wake cycle and in learning and memory. Alterations in TCEP histamine levels are closely connected with central nervous system dysfunction, and are thought to contribute to neurological disorders, including Alzheimer's disease and depressio
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It is noticeable that CO as
2022-01-13
It is noticeable that CO as well as H. pylori suppresses apoptosis while it induces autophagy in AGS cells. The differential effects of CO on the activation of transcription factors responsible for regulating expression of apoptosis- and autophagy-related genes merit further investigation. In concl
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br Conclusion br Conflict of interest
2022-01-13
Conclusion Conflict of interest References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Free fatty acids (FFAs) are essential nutrients that contribute to various cellular functio
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br Materials and methods br
2022-01-13
Materials and methods Results Using an 84 gene Th1-Th2-Th3 cytokine profile, 17 genes were significantly up-regulated in PBMC one week post-marathon compared to pre-marathon samples (Table 1). Eight genes were down-regulated among various subjects but none consistently enough to achieve statis
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It was noted elsewhere that
2022-01-13
It was noted elsewhere that several of the variants (i.e., Indel19 and SNP63) that make up the risk haplotypes had unusually large differences in allele frequencies between Africans and non-Africans, as compared with a set of likely neutral loci (Fullerton et al. 2002). This finding was interpreted
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