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Vortioxetine is a multimodal antidepressant that acts as
2024-08-17

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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Pituitary adenylate cyclase activating polypeptide PACAP is
2024-08-17

Pituitary adenylate cyclase-activating polypeptide (PACAP) is a member of the secretin/growth hormone-releasing hormone (GHRH)/vasoactive intestinal peptide (VIP) family, with potent anti-inflammatory and potent cytoprotective properties [[6], [7], [8], [9], [10], [11], [12], [13]]. PACAP exists as
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Some of the studies reported elevated ADA levels in
2024-08-17

Some of the studies reported elevated ADA levels in schizophrenia patients (SZ) undergoing treatment with antipsychotics (Dutra et al., 2010; Brunstein et al., 2007; Ghaleiha et al., 2011). However, it is unclear whether the increased serum ADA reported in these studies was the consequence of treatm
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AdK as an important upstream regulator
2024-08-17

AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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br Introduction Fungi are an inexhaustible source of
2024-08-17

Introduction Fungi are an inexhaustible source of natural products mainly due to their wide distribution in the nature, estimated to range from 1.5 to 5.1 million species in the world [1]. Secondary metabolites from fungi represent a substantial fraction of drugs and drug models in pharmaceutical
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Qualitative inspection of the single channel traces presente
2024-08-17

Qualitative inspection of the single-channel traces presented in both Figures 3 and 4 shows that within bursts of activity, βAnc-containing AChRs display a marked reduction in open probability. To quantify these differences in single-channel behavior, we performed dwell-time analysis under high-reso
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The lanthanide series of chemical elements comprises the
2024-08-17

The lanthanide series of chemical elements comprises the fifteen metallic chemical elements with atomic numbers 57 through 71, from lanthanum to lutetium. Though originally described as ‘‘rare earths’’ because of their natural occurrence as metal oxides, they are not particularly rare. The lanthanid
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Finally Urban Ciecko et al asked whether this enhancement
2024-08-17

Finally, Urban-Ciecko et al. (2018) asked whether this enhancement is specific to the pyramidal to SST neuron synapses or more generally observed in other synapses of the cortical microcircuit. Synapses between pyramidal cells showed no sign of potentiation after either bath application of the choli
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Steroidal CYP inhibitors can further be classified
2024-08-17

Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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The diagnosis of ICP is currently
2024-08-17

The diagnosis of ICP is currently based on the presence of pruritus, raised fasting serum TBS levels above 10μmol/L, and/or elevated serum transaminases (in the absence of diseases that cause cholestasis or pruritus) as well as spontaneous relief of signs and symptoms within four to six weeks after
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The original Aurora kinase was identified during a
2024-08-17

The original Aurora kinase was identified during a phenotypic screen for defects in mitotic spindles in Drosophila mutants. Aurora mutants were so named because of the morphological defects at the mitotic spindle resembling the Aurora borealis, or the Northern light [4]. The structure of the Auroras
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We wanted to investigate the influence of substituents
2024-08-17

We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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br Declaration of interest br Funding
2024-08-17

Declaration of interest Funding Introduction The endocrine disruptor bisphenol A (BPA) is a high-production chemical used in several consumer products, including polycarbonate bottles, epoxy resins, dental sealants, and thermal paper receipts (Geens et al., 2012). Importantly, BPA monomers
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br Future directions outlook Peptide based macrocycles are a
2024-08-16

Future directions-outlook Peptide-based macrocycles are among the privileged scaffolds in antibiotic drug discovery. Many compounds were discovered by natural product screening and developed unchanged, or as semi-synthetic derivatizations. Since the golden age of antibiotic discovery (1940s-mid 1
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br Regulation of AHR Activity AHR activity
2024-08-16

Regulation of AHR Activity AHR activity is regulated in various ways. First, AHR protein levels are controlled via ubiquitin-mediated proteosomal degradation: Ligand binding induces AHR ubiquitination and subsequent degradation by the proteasome [5]. AIP, a component of the AHR chaperone complex,
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