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br Experimental procedure br Funding The present study was s
2024-03-26
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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Given the profound expression of
2024-03-26
Given the profound brompheniramine maleate of 5-HT1A and 5-HT2A in the hippocampal CA1 region, and their potential to complex with mGluRs, the objective of this study was to examine if sleep deprivation alters the expression of 5-HT1A and 5-HT2A receptors and determine whether potential changes are
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-03-26
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Systematic administration of ABT amino bromophenyl morpholin
2024-03-26
Systematic administration of ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl) pyrido[2,3-d] pyrimidine), a potent and selective non-nucleoside AK inhibitor, also generates analgesic effects in animal models of pain (Jarvis et al., 2000, Kowaluk et al., 2000, Suzuki et al., 2001), sug
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In order to increase the oral bioavailability abiraterone
2024-03-26
In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral primaquine phosphate mg of abiraterone acetate (156), it is recommended that this drug should b
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Apelin is a peptide hormone and an endogenous ligand
2024-03-25
Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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MMP is the most critical protease which is involved in
2024-03-25
MMP9 is the most critical protease which is involved in the degradation of ECM. TIMP-1 is an important regulator in the synthesis and degradation of ECM [8,9]. Hepatic TIMP-1 expression significantly increases in patients with liver fibrosis [10]. Serum level of TIMP-1 expression is positively assoc
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The current antifungal pipeline contains several categories
2024-03-25
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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The reception of antiangiogenic treatment
2024-03-25
The reception of antiangiogenic treatment in neuro-oncology has yet to achieve the wide success rapidly accomplished for other malignancies. In 1984, mutated receptor tyrosine kinase became a culprit for aberrant tumorigenesis signal, providing a target for monoclonal Ceftazidime mg (mAbs) and smal
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Since non lipoprotein derived free cholesterol is recycled f
2024-03-25
Since non-lipoprotein-derived free cholesterol is recycled from the plasma membrane through the endosomal system through receptor-independent mechanisms, we wanted to determine whether ABCA2 could alter the trafficking of this source of free cholesterol. Our approach was to measure the effect of mob
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Adiponectin also works on AdipoR inducing extracellular Ca
2024-03-25
Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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Regarding androgens it is known that
2024-03-22
Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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Based on the observation that antipsychotic drugs
2024-03-22
Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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npy receptor Because serum ATX activity and
2024-03-22
Because serum ATX activity and npy receptor LPA are well correlated with liver fibrosis stage histologically, both of these parameters merit consideration as novel markers of fibrosis. However, serum ATX activity may be a more useful test from a clinical laboratory perspective. First, LPA can incre
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To maintain ATP levels postmortem muscle mobilizes its glyco
2024-03-22
To maintain ATP levels, postmortem muscle mobilizes its glycogen reserves to yield elastase inhibitor 6-phsphate that proceeds through glycolysis. Glycogen degradation was affected by the interaction between treatment and time (Pinitiation of the experiment. We expected that if myosin ATPase is li
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