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In addition to the above mentioned synaptic mechanisms the
2023-01-29
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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br Funding This work was supported by Arena
2023-01-28
Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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Structure activity relationships biochemical metabolic and m
2023-01-28
Structure–activity relationships [23], [24], [25], [26], biochemical [24], [25], [26], [27], [28], [29], [30], [31], metabolic [19], [27], [28], [29], [30], [31], and molecular [32] investigations have demonstrated that the substrate specificity, as well as other characteristics of T. gondii adenosi
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Firefly Luciferase mg Glucose permeability studies demonstra
2023-01-28
Glucose permeability studies demonstrated a high glucose flux through the SF films used in the present work. Recent diffusion studies, including small molecular drugs and oxygen permeation through SF membranes [32], further support the quality of SF and its possible application as a material for bio
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Furthermore new strategies to achieve a total androgen
2023-01-28
Furthermore, new strategies to achieve a total androgen deprivation namely by blocking either androgen biosynthesis as well as AR are being considered and should be a relevant topic in the near future. A successful example of this approach is galeterone (159), which not only inhibits the CYP17 enzym
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exemplifies three of the compounds investigated in
2023-01-28
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC RG7388 as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products. As BL
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l Arginine supplementation was reported to be efficient
2023-01-28
l-Arginine supplementation was reported to be efficient, inefficient or toxic in aged patients. The present study does not support our hypothesis that increased tissue arginase activity may account for the ineffectiveness and even the toxicity of l-arginine supplementation in ageing. Indeed, except
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Citral or dimethyl octadien al is a
2023-01-28
Citral or 3,7-dimethyl-2,6-octadien-1-al is a mixture of two stereoisomeric monoterpene aldehydes (the trans isomer geranial, citral A (40–62%)) and the cis isomer neral, citral B (25–38%) and serves one of the main constituent of essential oils of C. citratusis used in cosmetic, food, fungicides, p
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br The role of apelin in hepatic diseases
2023-01-28
The role of apelin in hepatic diseases The involvement of the apelin/APJ system in liver physiology and pathology has been proven in numerous studies (Table 6). For instance, in the experiment of Emam et al. [63] on rats suffering from hepatic injury, apelin decreased the levels of ALT, AST and L
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br Introduction Breast cancer is the second
2023-01-28
Introduction Breast cancer is the second most lethal cancer among women, accounting for approximately 40,000 deaths in the United States in 2015 [1]. The prognosis of breast cancer has improved significantly with the identification of immunohistochemical subtypes that predict response to therapy
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BX795 br Conflicts of interest br Funding br Introduction Br
2023-01-28
Conflicts of interest Funding Introduction Brassicaceae is an economically important family of plants containing rapeseed, cabbage, broccoli, brussels, radish and mustard. Among them rapeseed plays a crucial role, because of its application in food and also in fuel industry. According to th
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br Mortality and morbidity Alzheimer
2023-01-27
Mortality and morbidity Alzheimer's disease is officially listed as the sixth-leading cause of death in the United States [208]. It is the fifth-leading cause of death for those age 65 and older [198]. However, it ACET may cause even more deaths than official sources recognize. Alzheimer's is al
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Numerous studies have shown that PUFA
2023-01-27
Numerous studies have shown that ω-3 PUFA incorporation into the lipid raft can affect the distribution and function of protein in the lipid raft by altering raft composition [25], [26], [27]. For example, DHA treatment excluded phospholipase D (PLD) from lipid raft toward non-lipid raft, resulting
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2-Deoxyadenosine 5-diphosphate A selected set of these
2023-01-27
A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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br Conclusion Biotransformation of trachyloban oic acid by S
2023-01-26
Conclusion Biotransformation of trachyloban-19-oic ap5 by S. racemosum provided three products. Oxidation of compound 1 at C-17 (2–3), as well as rearrangement of 1 into a kaurane diterpene hydroxylated in C-16 and C-17 (4) were crucial for increasing AChE inhibitory activity. Compound 3 was mor
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