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We also noticed that acetic acid
2022-08-12

We also noticed that acetic acid by itself (used to induce pain) increased spinal cord levels of KYNA (see Fig. 5). The most rational explanation of this finding is based on the possibility that acetic acid and KYNA share the same transport systems and the finding is therefore not surprising. Altho
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br Conflict of Interest Both GM and BDH
2022-08-12

Conflict of Interest Both GM and BDH are shareholders in Caldan Therapeutics, a company exploring potential novel treatments for type 2 diabetes. Acknowledgments Work described herein was supported by Biotechnology and Biological Sciences Research Council [grant BB/K019864/1)] (to GM) and [gr
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br Next we explored the SAR around
2022-08-12

Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic old town sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did no
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The aim of this study is to explore new Glo
2022-08-12

The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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The amino hydroxy methyl isoxazolepropionic acid AMPA recept
2022-08-12

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic corticotropin releasing factor (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with Glu
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In conclusion we have designed and
2022-08-12

In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date, m
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The discovery that GLUT in the microvasculature represents a
2022-08-12

The discovery that GLUT1 in the microvasculature represents an important target of VEGF thereby affecting 2-Deoxycytidine function is highly relevant. The work of Jais et al. identified VEGF as a determining player in the regulation of cognitive performance and provides an important link to the unf
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Historically a role for the prefrontal
2022-08-12

Historically, a role for the prefrontal cortex in spatial working memory has been repeatedly claimed (for review, see Kolb, 1984). Older studies using traditional, non-fibre-sparing lesions (e.g. aspiration lesions) often resulted in spatial alternation deficits. In contrast, more recent studies emp
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Since the isoflavone emerged as privileged scaffold in
2022-08-12

Since the isoflavone emerged as privileged scaffold in Hh inhibition, based on molecular modeling predictions and prior studies [17,22], here we designed a number of isoflavones able to interact preferentially with the Smo receptor or the Gli protein. Molecules were synthesized by means of a novel s
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Previously we have shown that
2022-08-12

Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo
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br Novel mechanisms of fipronil resistance
2022-08-12

Novel mechanisms of fipronil resistance in planthoppers Conclusion Conflict of interest Introduction Methamphetamine, a widely abused drug, is mainly used as a psychostimulant although it is occasionally used at low doses for medical purposes, such as in attention deficit or hyperactivit
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br Although earlier studies had reported conflicting results
2022-08-11

Although earlier studies had reported conflicting results regarding the role of Ca2+ in regulating SV endocytosis, more recent data suggest that Ca2+ influx facilitates SV endocytosis in hippocampal neurons, the calyx of Held, and in inner hair RVX-208 mg (Dittman and Ryan, 2009, Hosoi et al., 20
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The H R antagonist JNJ developed by Johnson Johnson
2022-08-11

The H3R antagonist JNJ-17216498, developed by Johnson & Johnson, has entered clinical trial studies, but no information regarding its structure has been publicized to date. A phase II study of JNJ-17216498 monotherapy has been completed for patients with narcolepsy, but the results are not publicall
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UCB 35625 There were hub genes identified by WGCNA among
2022-08-11

There were 11 hub genes identified by WGCNA among which KIBRA was the hub gene of the black module. The bioinformatics method is an effective and powerful tool to analyze mRNA UCB 35625 profiles and the related pathways. For instance, the lung cancer risk modules that were closely related to lung c
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Here we examine the impact of
2022-08-11

Here we examine the impact of hypoxia on lake whitefish (Coregonus clupeaformis) during embryonic and larval development. Lake whitefish are a cold-water salmonid endemic to North America and are found from western Alaska, USA to eastern Labrador in Canada. Spawning occurs from late autumn to early
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