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The other possibility for the lack of
2021-11-17
The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,
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br Main Text Metabolism drives diverse biological processes
2021-11-17
Main Text Metabolism drives diverse biological processes including differentiation, proliferation, and effector function in diverse cell types. In particular, the process of mounting an innate immune response to pathogens entails rapid sensing of a wide range of patterns displayed by invading mic
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There is evidence for an adverse sympatho stimulatory effect
2021-11-17
There is evidence for an adverse sympatho-stimulatory effect in the medulla oblongata mediated by the α1/β1 isoform, implying a possible benefit of selective α2/β1 activation [19]. While the stimulator BAY 41–2272 increases NO-sensitivity of both isoforms [20], a prevalence of the α1/β1 isoform comp
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The elective controlled fasting study in our patient provide
2021-11-16
The elective controlled fasting study in our patient provides further metabolic profiling in patients with GCGR defect. Despite her lean body mass with low weight, at the age of 7 years old she demonstrated a good tolerance for fasting with hypoglycemia Benzoylmesaconitine australia level, insulin,
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According to the aforementioned preclinical and
2021-11-16
According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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Ghrelin contains an n octanoylation at its
2021-11-16
Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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bicuculline Fig a and b illustrates a slow inhibition
2021-11-16
Fig. 3a and b illustrates a slow inhibition by PMA in 2 μM Ca2+. Moreover, channel inhibition was reversed by addition of PKC19–31, a peptide inhibitor specific for PKC, as shown in Fig. 3c. In three experiments, Im was reduced to 14.5±0.6% of the control value by PMA to increase to 207.6±73.6% by a
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The conversion of lactose to GOS by gal involves the
2021-11-16
The conversion of lactose to GOS by β-gal involves the same transglycosylation mechanism used by most glycoside hydrolases (GHs). This mechanism (Fig. 1) involves an enzyme-bound intermediate and consists of two processes: glycosylation and deglycosylation (Adlercreutz, 2017). The glycosylation proc
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There are additional implications of subunit alterations
2021-11-16
There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure
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The extensive worldwide research efforts in the decade
2021-11-16
The extensive worldwide research efforts in the decade following FFA1 de-orphaning aimed at developing clinically useful FFA1 agonists were nearly halted after Takeda’s first-in-class agent fasiglifam (TAK-875) was discontinued in phase III of human trials. On the date of submission of this manuscri
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During the activation of the coagulation cascade factor Xa F
2021-11-16
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium Meptazinol HCl on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit
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The FAAH inhibitor activity of the ethoxycarbonyl phenyl
2021-11-16
The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound
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br Acknowledgement This research was supported by Basic Scie
2021-11-16
Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral GSK2334470 is the most popular administration route due to good patients’ co
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The finding that a peptide
2021-11-16
The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino TAK-875 receptor ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1
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It has been demonstrated that HO inhibits the
2021-11-16
It has been demonstrated that HO-1 inhibits the production of proinflammatory mediators including TNF-α and IL-6 in response to sepsis [35], and the expression of iNOS and COX-2 [36,37]. An inverse association between HO-1 and iNOS has previously been described: the NO levels decline with increases
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