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An alternative to the agonist
2024-09-21

An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Fig A shows a schematic representation of histological
2024-09-21

Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the
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br Author contributions br Conflicts of interest
2024-09-20

Author contributions Conflicts of interest The authors declare no competing financial interests. Acknowledgement This work was supported by grants from the Deutsche Forschungsgemeinschaft (Sonderforschungsbereich/Transregio 166–Project C1 and grant CA 1014/1-1 to D.C.) and the IZKF Würzbur
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Furthermore low affinity sites that share no structural homo
2024-09-20

Furthermore, low-affinity sites that share no structural homology with the aforementioned sites have been described in the transmembrane domain. It has been discovered that, in α1βγ2 receptors, potentiation of GABA-activated currents by high concentrations of diazepam is biphasic, with a high- and a
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Over expression of the inflammatory cytokines MMPs
2024-09-20

Over expression of the inflammatory cytokines, MMPs and COX-2 act as an important inducer of chronic inflammation. COX-2 catalyzes the biosynthesis of prostaglandins (PGs), and induced expression was observed in Tylosin phosphate sale stimulated with pro-inflammatory cytokines or bacterial lipopoly
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HMGA proteins have also been linked
2024-09-20

HMGA proteins have also been linked to localized changes in chromatin/nucleosome structure and alterations of cellular phenotype during induction of gene transcription in activated T lymphocytes. An adaptive immune response is initiated when naïve resting T lymphocytes encounter their corresponding
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br Angiotensin receptor neprilysin inhibitors Sacubitril val
2024-09-20

Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu
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br Material and methods br Results br Discussion
2024-09-20

Material and methods Results Discussion Although we were not able to detect 12/15-LOX mRNA in the lungs of 12/15-LOX knockout mice substantial amounts of 15-HETE could be detected in BALF. In fact, significant synthesis of 15-HETE in 12/15-LOX mice have been already reported [17]. The redun
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We found evidence of the interaction between AR and
2024-09-20

We found evidence of the interaction between AR and hemiacetals by evaluating the effect of glucose on l-idose reduction. l-idose was recently proposed as the best AR substrate able to mimic glucose [38]. This aldose is structurally very closely related to d-glucose, from which it differs only in th
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br Acetaldehyde One of the most common http
2024-09-20

Acetaldehyde One of the most common environmental aldehydes is acetaldehyde (CH2CHO). Acetaldehyde, which is highly volatile, has been classified as a Group I human carcinogen by the International Agency for Research on Cancer [30]. Aldehydes can form DNA adducts, including ring-open forms of cro
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Both subcutaneous s c and
2024-09-19

Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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Casein accounts for of the total protein
2024-09-19

Casein accounts for 80% of the total protein in bovine milk (Capriotti, Cavaliere, Piovesana, Samperi, & Laganà, 2016); hydrolysates or bioactive peptides derived from casein have been employed widely in food as a functional ingredient (Capriotti et al., 2016, Field et al., 2008). Many studies have
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The reaction of LOX with unlabeled AA generated products fro
2024-09-19

The reaction of 5-LOX with unlabeled AA generated products from hydrogen abstraction at C7 (95% 5-HETE) with minor products derived from abstraction at C10 (5% 8-HETE). With 7,7--AA the selectivity remained skewed towards C7 hydrogen abstraction (59%) compared to C10 hydrogen abstraction products (4
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The syntheses of a and b
2024-09-19

The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each SC75741 australi
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br Role of autophagy in
2024-09-19

Role of autophagy in alcoholic cardiomyopathy Concluding remarks The genetic and phenotypic heterogeneity in alcoholic cardiac injury has been recognized despite the seemingly beneficial effects of low to moderate alcohol consumption [8]. Although oxidative stress is well established in the pa
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