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The first suggestion that histamine may play a role in
2021-10-20

The first suggestion that histamine may play a role in memory consolidation was from Almeida and Izquierdo (de Almeida & Izquierdo, 1986) who showed that the immediate posttraining intracerebroventricular (i.c.v.) administration of 1–10ng of the drug were found to enhance the retention of one-trial
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In an effort to further improve the intrinsic potency
2021-10-20

In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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To solve the atomic structures of several individual domains
2021-10-20

To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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In this study we further expanded the antitumor bioactivity
2021-10-20

In this study, we further expanded the antitumor bioactivity, with the BALB/c S-180 tumor model, which is long-established due to its highly aggressive in all strains of laboratory mice and rats (Cui et al., 2003). We investigated the tumor-regressing ability of β-glucan by different modes of admini
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Although the overall structures of mGlu
2021-10-20

Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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br Regulation of Glu transporters The pivotal role of
2021-10-20

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino MCB-613 calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcriptio
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In the present study five Glu substituted analogues of GIP
2021-10-19

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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The eradication of agonist activity
2021-10-19

The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary Hydrocortisone as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagon
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One effective approach to fine tuning
2021-10-19

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Irinotecan HCl Trihydrate scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3
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PKC s effect on quantal size may involve regulation of
2021-10-19

PKC’s effect on quantal size may involve regulation of endocytotic protein components responsible for mediating kiss-and-run exocytosis. There is a growing body of evidence to suggest that canonical endocytotic proteins—dynamin, amphiphysin, syndapin, and others—may play a role in modulating fusion
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While IN inhibitors are a relatively new addition
2021-10-19

While IN inhibitors are a relatively new addition to the clinician's palette of drugs to formulate HAART regimes, resistance to both INSTIs and LEDGINs has been observed. For example, even within Australia where it is estimated that 25,313 people are currently living with HIV and the infection rate
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br Results and Discussion The Set sequence is homologous to
2021-10-19

Results and Discussion The Set7 sequence is homologous to the other identified histone methyltransferases in S. pombe (Figure S1) and also shares similarity with human HMTases, H3K9 GLP/Ga9, and H4K20 SUV420H1 (Figure S1). Set7 fused with the GFP (Set7-GFP) localized in the nucleus and cytoplasm
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In conclusions it is hypothesized that caffeine administrati
2021-10-19

In conclusions, it is hypothesized that caffeine administration could lead to an increase in histamine neuronal activation or release of histamine [38] to induced locomotor stimulation via H1 receptor activation. In addition, the present study also propose that the spaced administration of caffeine
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Intracellular signaling pathways leading to IR
2021-10-19

Intracellular signaling pathways leading to IR injury are initiated by an increase in reactive oxygen species (ROS). This occurs principally at the time of initiation of reperfusion, which is accompanied by the re-admission of oxygen to the ischemic tissue. The resulting cascade of downstream events
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Taken together our results indicate that HSF
2021-10-19

Taken together, our results indicate that HSF1 and NRF2 reciprocally regulate HO-1 expression. Although each of HSF1 and NRF2 controls a distinct cytoprotective pathway, mounting evidence points that they engage in crosstalk [15,22]. The protein-protein interaction between HSF1 and NRF2 may be inter
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