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The physiological and pharmacological roles of
2022-01-13

The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po
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br Conclusion and future perspectives The nicotinic
2022-01-13

Conclusion and future perspectives The nicotinic 2-D08 receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid and la
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GPR has been implicated in neuropathic and inflammatory
2022-01-13

GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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It appears that not all GPR agonists require
2022-01-13

It appears that not all GPR119 agonists require a high dose to elicit acceptable PRIMA-1 synthesis control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/
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Because of the commercial availability of some
2022-01-13

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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The first hypothesis better fertility in heifers
2022-01-13

The first hypothesis, better fertility in heifers that had CL at day 0, was clearly supported by our results. Heifers with a CL had over 60% P/AI compared to ∼50% in heifers without CL. These results are consistent with several other studies reporting that cycling heifers have greater fertility tha
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In this study three potential Otx binding sites were
2022-01-13

In this study, three potential Otx-2 Deacetylase Inhibitor Cocktail were found in the promoter region of the sheep GnRH gene: −1786 bp to −1770 bp, −825 bp to −819 bp, and − 529 bp to −523 bp. Combined with the results of the double-luciferase assay, it could be inferred that the binding site of Ot
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In parallel we were also
2022-01-13

In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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br Material and methods br Results br Discussion Organisms h
2022-01-13

Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In Nilvadipine to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver [19]. This s
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Another group of secreted proteins that
2022-01-13

Another group of secreted proteins that determine the virulence of V. dahliae are effectors and microbe associated molecular patterns (MAMP) that regulate plant immunity [10]. So far, there is only one Nimodipine gene Ave1 cloned in V. dahliae, yet it does not exist in race 2 strains such as V592 a
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To synthesize the azaindole based compound Suzuki coupling o
2022-01-12

To synthesize the 7-azaindole based compound , Suzuki coupling of 6-chloro-7-azaindole with 4-CFO-phenylboronic Nicardipine HCl was carried out in the presence of Pd(dppf)Cl·CHCl to supply biaryl in quantitative yield (). Iodination at the C-3 position resulted 3-iodo-7-azaindazole . Alkylation of t
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In the present study five Glu substituted analogues of GIP
2022-01-12

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Due to the versatility of the ghrelin system and its
2022-01-12

Due to the versatility of the ghrelin system and its multiple functions, dysregulation in some of the components of the ghrelin system, such as ghrelin, GOAT, and GHSR, might lead to pathogenesis of many endocrine-related diseases, including obesity, short stature, cancer, inflammatory, and cardiova
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Among sensitizers tested in the previous study six test
2022-01-12

Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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The F P concentration reported for a resting
2022-01-12

The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase
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