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To discriminate the peripheral and central involvement
2022-01-04

To discriminate the peripheral and central involvement of FAAH in paracetamol action, we proposed a pharmacological strategy challenging the analgesic action of paracetamol observed in an inflammatory context with either a peripherally-restricted FAAH inhibitor (URB937, Clapper et al., 2010, Moreno-
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Recent findings of us suggest
2022-01-04

Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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br Materials and methods Male Sprague Dawley rats Faculty
2022-01-04

Materials and methods Male Sprague–Dawley rats (Faculty of Pharmacy, Pharos University, Alexandria, Egypt) weighing 180 to 200g were used in this study. All experiments were performed in strict accordance with institutional animal care and use guidelines. Results Discussion The current stu
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The only approved H R antagonist inverse agonist is
2022-01-03

The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or
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Toc and Toc are GTPases that regulate
2022-01-03

Toc34 and Toc159 are GTPases that regulate initial steps of preprotein import [3,4,26]. It was shown that GTP hydrolysis of at least one receptor is necessary to initiate the translocation process [23,27]. As reported for other small G-proteins, Toc34 and Toc159 bind their cargo in a nucleotide-depe
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In this study we demonstrated that while
2022-01-03

In this study, we demonstrated that while Cu(I) does not affect LPS induced iNOS conotoxin mg it inhibits NO release from microglia. Cu(I)-induced GSNOR inhibition and GSNO depletion is more in line with alternative (non-inflammatory) polarization. These results extend our previous findings that Cu(
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Pam3CSK4 receptor Firstly the impact on activity and
2022-01-03

Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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With taurine or other molecules that might be
2022-01-03

With taurine, or other molecules that might be transported by Eaat2, an important area of research will be how such a chemical regulates sleep. Indeed, taurine has been described to act on the nervous system in disparate ways — it can act as an inhibitory neurotransmitter, but also has a well-charac
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To further implicate the role
2022-01-03

To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 nearly was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-type mice at 2
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To support maximal growth and metabolic function of major
2022-01-03

To support maximal growth and metabolic function of major organs, glucose and apexbt kinase inhibitor are essential. We assessed the plasma levels of glucose and amino acids in LBW and NBW piglets at birth and at day 7 postpartum. Blood glucose levels were influenced by birthweight and age. In this
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GHRL effect on appetite is influenced by
2022-01-03

GHRL effect on appetite is influenced by its dose and route of administration, where central or peripheral administration of GHRL at low doses increases feed intake, via acting on orexigenic hypothalamic neurons, and decreases appetite at high doses in chickens (Jonaidi et al., 2012), quails (Shoush
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The PK profile and tissue distribution of which has biologic
2022-01-03

The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an
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GLP is released in response to
2022-01-03

GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty leukotriene b4 receptor receptor 4 (FFA4/GPR120) as a potential 7TM recepto
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calculate molarity of a solution Stability of DBS over the d
2021-12-31

Stability of DBS over the 60-day time points was encouraging, with a maximum of 0.1 log10 IU/mL degradation from the day 1 value (Supplementary Fig. 1 and Supplementary Table 3). Discussion This study evaluated the sensitivity and specificity of the Aptima HCV Dx assay for HCV RNA detection from
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br Intracellular trafficking with concurrent
2021-12-31

Intracellular trafficking with concurrent signaling of NPRA Our recent studies have shown internalization and concurrent signaling of NPRA in subcellular compartments; this had not been previously demonstrated [26,42]. Preparation of the enhanced GFP (eGFP)-tagged NPRA (eGFP-NPRA) construct has g
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