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From our in vivo studies and
2024-01-24

From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar
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br The role of apelin in hypertension diseases
2024-01-24

The role of apelin in hypertension diseases The role of apelin and its receptor APJ in cardiovascular diseases has been described in numerous studies (Table 2) [36,37]. It has been revealed that exogenous apelin may lower blood pressure. Tatemoto et al. [6] have discovered that different forms of
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Another interesting aspect of neutralizing
2024-01-24

Another interesting aspect of neutralizing AP-1 is the inhibition of interactions between AP-1 and Smad proteins, which synergize to activate the TGF-β1-responsive genes involved in hypertrophic growth of the heart muscle and in the development of cardiac fibrosis. Through preventing AP-1 activation
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In spite of this unexpectedly
2024-01-24

In spite of this, unexpectedly, after three-week cherry puree consumption no AC increase was observed, irrespective of the method used (Table 2). A statistically significant decrease of AC was even measured by LOX-FL and ORAC methods (−3.5% and −9%, respectively). Nevertheless, a much more evident d
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br Acknowledgments This work was supported by a grant of
2024-01-24

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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We next considered the effect of
2024-01-24

We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga
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Herein we employ an adapted
2024-01-24

Herein we employ an adapted targeted quantitative proteomic isotope dilution method, developed in our laboratory [[18], [19], [20], [21]], to quantify membrane transporters in fresh lung from five donors, in four immortalized human lung cell lines and in three control cell lines. We quantify twelve
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br Transparency document br Introduction G protein
2024-01-24

Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and
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Introduction Adenosine monophosphate cAMP is a
2024-01-23

Introduction Adenosine 3′,5′-monophosphate (cAMP) is a general-purpose signaling molecule present in most branches of life. Intracellular cAMP levels control diverse cellular functions. In bacteria, cAMP regulates metabolism by activation of the catabolite activator protein (CAP), also known as cAM
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In the isolated right atrium activation of muscarinic recept
2024-01-23

In the isolated right atrium, activation of muscarinic receptors and adenosine receptors may block the generation of action potentials in the sinoatrial node, inducing cardiac arrest (Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5) (Camara et al., 2015, Campbell et al., 1989). Physiologically, this conditio
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The cytoplasmic domain of muscle AChR is not accessible
2024-01-23

The cytoplasmic domain of muscle AChR is not accessible to adefovir in vivo. Theoretically, therapy with the cytoplasmic domains should be safe. Safety is demonstrated by the facts that: (1) rats repeatedly immunized with the cytoplasmic domains in TiterMax adjuvant do not develop EAMG, although th
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Vortioxetine is a multimodal antidepressant that acts as an
2024-01-23

Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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Additionally regulation of GPCR heteromerization by
2024-01-23

Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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Given these findings above we hypothesized that
2024-01-23

Given these findings above, we hypothesized that hypernociception produced by intra-amygdala 8-OH-DPAT is result of hyperpolarization in this area. This neuronal inhibition of the amygdaloid complex might result in an inactivation of crucial neurotransmitter systems of the descending inhibitory pain
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lgk974 br Materials and methods br
2024-01-23

Materials and methods Results Discussion Prostate cancer represents an ideal candidate for chemoprevention because of its high incidence and long latency to clinically significant disease [17]. The precancerous lesion PIN may also be a suitable target for ablation in chemoprevention strateg
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