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Several studies have found that GPR
2022-04-06

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected α-Cyperone expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (R
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The synthesis of nitropyrimidine analogs was outlined in
2022-04-06

The synthesis of 5-nitropyrimidine analogs – was outlined in . 4,6-Dichloro-5-nitropyrimidine, 4-methylsulfonylaniline and 2-fluoro-4-methylsulfonylaniline were prepared according to previously reported procedures., , Reaction of 4,6-dichloro-5-nitropyrimidine and substituted aniline in DMF yielded
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Initial evidence that cell contact mediated transmission of
2022-04-06

Initial evidence that cell-contact-mediated transmission of HIV-1 is relevant for the generation of latently infected Levonorgestrel was suggested in the context of transmission from dendritic cells to resting CD4+ T cells (Evans et al., 2013, Kumar et al., 2015). As dendritic cells probe for antig
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To further investigate its role in stresses tolerance OsGly
2022-04-06

To further investigate its role in stresses tolerance, OsGly I was overexpressed in transgenic rice. qRT-PCR and zymologic determination showed that Z-VEID-FMK synthesis level of OsGly I and the glyoxalase I activity were significantly increased to different extent in the transgenic overexpression
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One possible pathway summarizing the overall action
2022-04-06

One possible pathway summarizing the overall action involves NMDA receptor activation – Ca2+ influx – protein kinase A (PKA) activation – ERK phosphorylation and subsequent synaptic plasticity (Thomas and Huganir, 2004). A few studies have also shown modulation of synaptic glutamate transporters in
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Results indicated that superfusion of orexin alone glutamate
2022-04-06

Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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Having shown that some of
2022-04-06

Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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Post translational modifications of the GR can alter
2022-04-06

Post-translational modifications of the GR can alter the transcriptional effects of GR activation [31], and may provide a mechanism for the interactions between cell signaling pathways and GR-mediated transcriptional activity. Dex-BSA treatment reportedly increased p38 MAPK activation in CD14-positi
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br Conclusion br Conflict of Interest JJH
2022-04-06

Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant
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4EGI-1 receptor br Secretase modulators a loss
2022-04-06

γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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In the course of our ongoing
2022-04-06

In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric CPI-169 type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the process
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br Summary The presented results of the analysis of the
2022-04-06

Summary The presented results of the analysis of the unfolding of G-quadruplex and i-motif, which may appear within the telomeric DNA region, led to several important conclusions. Namely, determination of the work necessary to unfold of these structures, in biased molecular dynamics involving ste
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The overall very satisfactory potency profile
2022-04-06

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Epibrassinolide core in order to improve affinity to FFA1. The agonist activity in this series appears to be particular
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In contrast with the above results in our
2022-04-06

In EW-7197 with the above results, in our GC model system, FPR1-, but not FPR2-knockout, enhanced tumour formation. However, it should be noted that the prominent role of mFPR2 with respect to mFPR1 in the mouse colon might be due to the significantly higher expression of mFPR2 than mFPR1 in this t
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br Material and methods br Results br Discussion In
2022-04-06

Material and methods Results Discussion In the present study, we attempted to unravel the mechanism underlying the statin-mediated inhibition of FGFR3 signaling in chondrocytes, reported earlier by Yamashita and colleagues. We evaluated the role of statins in four different experimental sys
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