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Among all the compounds the novel L
2024-06-19

Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The SBE 13 HCl 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91 nM) and
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PAN induced nephrosis was accompanied
2024-06-19

PAN-induced nephrosis was accompanied by loss of body weight, decrease of food intake, increase in urine volume and increases in triglycerides and cholesterol levels, which have been reported previously (Natori et al., 1996). Except for urine volume, each one of these measures was improved by A-3069
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The nAChR has been considered an interesting potential targe
2024-06-19

The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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Although our data failed to reproduce
2024-06-19

Although our data failed to reproduce the robust enhancement of LTP in the rat dentate with nicotine that was previously reported, our results with NS6740 suggest a more fundamental role for α7 receptor signaling in modulation of synaptic tone in the LTP pathway. The discovery of the cholinergic ant
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Introduction Chronic inflammation is increasingly known as o
2024-06-19

Introduction Chronic inflammation is increasingly known as one of the most critical etiological factors in gastrointestinal (GI) cancers (Lee et al., 2016; Wang and Cho, 2015). Overexpression of 5-lipoxygenase (5-LOX), 5-LOX-activating protein (FLAP), as well as other leukotriene (LT) biosynthetic
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Autotaxin has been linked to chemoresistance through its abi
2024-06-18

Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer kisspeptin [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-expressed in pati
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The canonical binding sites to which
2024-06-18

The canonical vasopressin receptor antagonists to which α2, α3, or α5 contribute are highly similar. Therefore, differences in ligand affinity will not be large even if a ligand makes optimal use of the small differences in the pockets. As a possible alternative approach to achieve separation of co
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Introduction Preeclampsia a serious hypertensive disorder th
2024-06-18

Introduction Preeclampsia, a serious hypertensive disorder that can occur during pregnancy, is a pregnancy-related disease characterized by the onset of p-nitro-Cyclic Pifithrin-α and proteinuria after the 20 t h week of gestation, and it occurs in about 5% of all pregnancies [1]. If left untreate
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Available data thus indicate that there
2024-06-18

Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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SNX-2112 Experimentally the ECD spectrum of showed three ECD
2024-06-18

Experimentally, the ECD spectrum of 1 showed three ECD bands: positive ones at 260 and 200nm, and a negative one at 230nm (Fig. 4). Meanwhile, there is only one broad positive ECD band starting from 300nm in the ECD spectrum of 2. ECD spectra of 1 and its derivatives attracted great interest because
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br Summary br Introduction With readily synthetic methods
2024-06-18

Summary Introduction With readily synthetic methods and excellent chemical/physical characteristics, coumarins have received extensive attention and show great practical values in many fields, such as medicine discovery, dye chemistry, materials chemistry and so on [[1], [2], [3]]. Actually, o
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In summary present evidence suggests that antimicrobial ther
2024-06-18

In summary, present evidence suggests that antimicrobial therapy for intra-abdominal sepsis can be shortened in patients exhibiting a clinical response to treatment. Hence, clinicians should use the resolution of clinical signs of infection as a guide to determine when during the 4–7-day window anti
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The most common grade AEs associated
2024-06-18

The most common grade 3/4 AEs associated with the soluble fusion protein ziv-aflibercept are neutropenia, hypertension, and diarrhea [63]. In general, medical oncologists associate ziv-aflibercept with worse toxicity than BV, and meta-analyses of clinical trial data with ziv-aflibercept or BV suppor
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br Experimental methods br Acknowledgments br Introduction L
2024-06-18

Experimental methods Acknowledgments Introduction Long-term potentiation (LTP) and long-term depression (LTD) at excitatory synapses are thought to underlie experience-dependent learning and memory. These synaptic plasticity mechanisms are best characterized at hippocampal CA1 synapses, whe
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br Acknowledgments This work was supported by a
2024-06-18

Acknowledgments This work was supported by a grant of the Romanian National Authority for Scientific Research, CNCS – UEFISCDI, project no. PN-II-ID-PCE-2011-3-0571, awarded to F.A.M. D.V.N. was co-financed from the European Social Fund through Sectorial Operational Program Human Resources Develo
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