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br Introduction Depressive disorder is a syndrome characteri
2021-11-02

Introduction Depressive disorder is a syndrome characterized by a group of heterogeneous symptoms that affect more than 350 million people worldwide, 4% of world population (WHO, 2012). The WHO estimates depression will be the leading global cause of disability in 2020, with tremendous economic c
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Some biguanides can cross the
2021-11-02

Some biguanides can cross the mitochondrial membrane and increase L-lactate formation by inhibiting oxidative SC75741 [34]. On the other hand, it has also been reported that levels of fasting plasma lactate in T2DM patients are similar regardless of whether or not metformin is administered [35] and
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Acknowledgments Financial support from the National
2021-11-02

Acknowledgments Financial support from the National Natural Science Foundation of China (81730094, 81473262 and 81573299) is gratefully acknowledged. This project was also supported by the “111 Project” from the Ministry of Education of China, the State Administration of Foreign Expert Affairs of C
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GnRH ant have been designed to obtain pharmacological compou
2021-11-02

GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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br The methyl aspartate receptor NMDAr hypofunction hypothes
2021-11-02

The -methyl--aspartate receptor (NMDAr) hypofunction hypothesis of schizophrenia correlates disease symptomology with glutamatergic neurotransmission dysfunction., , , Therefore, inhibition of glycine transporter 1 (GlyT1) to elevate synaptic levels of glycine and potentiate NMDAr signaling is a
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The glycine receptor is an ionotropic neurotransmitter recep
2021-11-02

The glycine receptor is an ionotropic neurotransmitter receptor coupled to a chloride ion channel. Glycine receptors are typically described as inhibitory and distributed in the spinal cord and brainstem, though mRNA transcription labelling studies in rats show expression in the hippocampus, cingula
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protease activated receptor In the present study we tested g
2021-11-02

In the present study, we tested α-glucosidase and tyrosinase inhibitory effects of the methanol extract from lower stems and protease activated receptor of Q. coccifera (1) as well as the isolated compounds [lyoniresinol-9-O-β-xylopyranoside (2) and lyoniresinol-9-O-β-glucopyranoside (3), coccifero
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In addition this study also showed
2021-11-02

In addition, this study also showed no obvious increase in apoptosis but obvious increase in necrosis after WZB117 treatment. The possible reason is that apoptosis is an ATP-utilizing process which is an active and programmed form of cell death. In contrast, necrosis is an uncontrolled or pathologic
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In conclusion we have shown that AKR
2021-11-02

In conclusion, we have shown that AKR1D1 regulates glucocorticoid availability and GR activation and therefore represents a key pre-receptor regulator of hormonal action in human liver. However, there are additional questions that need to be addressed including dissecting the broader role of AKR1D1
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br Calcium permeability pathway It has been demonstrated tha
2021-11-02

Calcium permeability pathway It has been demonstrated that physiological shear stress in the circulation causes a reversible increase in Ca2+ permeability [29], [30], [31], [32], [33] and electrophysiological evidence has been recently reported for transient activation of the Ca2+-sensitive K+ ch
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The overall decrease in consummatory drive seen in rodents
2021-11-02

The overall decrease in consummatory drive seen in rodents treated with naltrexone in previous studies is in accordance with the effects seen with mice treated with SNAP 37889 in this study. While it may seem inappropriate to use a broad-acting drug like SNAP 37889 that suppresses overall consummato
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Plasmid construction and site directed mutagenesis of M lute
2021-11-02

Plasmid construction and site-directed mutagenesis of M. luteus B-P 26 UPS. For the expression of N-terminus His6-tagged M. luteus B-P 26 UPS, the expression plasmid pMluUEX [7] was cleaved with the restriction enzymes NdeI/BamHI. The gene fragment was inserted into an NdeI/BamHI-treated pET-15b to
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br Acknowledgments R Dalmann has obtained a bourse
2021-11-02

Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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Current guidelines for thromboprophylaxis recommend the use
2021-11-01

Current guidelines for thromboprophylaxis recommend the use of vitamin K antagonists (eg, warfarin), low-molecular-weight heparin (LMWH), or indirect inhibitor of factor Xa . Aspirin is also used for thromboprophylaxis in patients undergoing orthopedic procedures , . The efficacy and safety of LMWH
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MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl
2021-11-01

MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr
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