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Fig illustrates the different signaling pathways elicited
2022-07-18
Fig. 1 illustrates the different signaling pathways elicited or modulated by H3R activation. Collectively, the modulation of the release of histamine and other neurotransmitters through H3R activation could be linked to several neurological disorders such as sleep disorders like narcolepsy, Alzheime
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Expression of p NTR has been linked
2022-07-18
Expression of p75NTR has been linked to several aspects of aggressive glioma growth, including migration and invasion, by various mechanisms in a large number of elegant studies [6], [7], [26], [27]. Our study adds to this literature by demonstrating specific roles in hypoxic tumor cells and regulat
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br Acknowledgments Work in SI s laboratory is supported by
2022-07-18
Acknowledgments Work in SI’s laboratory is supported by grant IM 20/4-1 from the Deutsche Forschungsgemeinschaft, Bonn (Germany) and grant EKFS 2012_A309 from the Else Kröner Fresenius Stiftung, Bad Homburg (Germany). FW’s group is supported by the Dr Vaillant Foundation and the Dutch Burns Found
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There are five main research findings regarding possible mec
2022-07-18
There are five main research findings regarding possible mechanisms of low-level HBsAg expression: Most of these findings are related to the use of antiviral therapy, which results in pre-S/S gene mutations, the development of occult hepatitis, the use of immunosuppressants or S gene methylation, b
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Substrate affinity and specificity can be
2022-07-18
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of AICAR bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of short li
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br For some time it was known that
2022-07-18
For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor PR-619 in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on the regulati
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The biological activity at GPR a of
2022-07-16
The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu
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It is possible that maternal separation induced USV
2022-07-16
It is possible that maternal separation-induced USV in neonatal rodents is not a good model of adult anxiety for examining GlyT1 inhibitors, if the expression levels of GlyT1, GlyA, and GlyB markedly differ between pups and adults. However, several reports provide evidence that this is not the case.
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Consistent with these observations impaired transduction
2022-07-16
Consistent with these observations, impaired transduction of the glutamate signal by NMDARs (i.e., NMDA receptor hypofunction [NRH]) by parvalbumin-containing GABAergic inhibitory interneurons is implicated in mediating social deficits, a domain of psychopathology responsible for poor functional out
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Azithromycin Dihydrate A number of experimental data declare
2022-07-16
A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in Azithromycin Dihydrate and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Behari and
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br Preclinical development of GIP agonists Since
2022-07-16
Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications a
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Serotonin hydroxytryptamine HT is a
2022-07-16
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the M344 as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and Condron, 2010;
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Tetrazole is one of the most commonly used bioisosteres for
2022-07-16
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive a
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As concerns TRPV assays benzylic amides and benzylic reverse
2022-07-15
As concerns TRPV1 assays, benzylic amides and benzylic reverse amides exhibited an overall superiority over their aryl counterparts and , and ureas and . A reversed trend was however observed with the 4-chlorostyryl and 4--butylphenyl moieties (compare compounds and ; , , and ; and ). The EC and IC
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We examined the expression of notch in
2022-07-15
We examined the expression of notch-1 in the brains of mice following morphine or oxycodone tolerance. The results showed that notch-1 levels did not change following morphine or oxycodone tolerance, with or without the treatment of IRL-1620. This indicates the possibility that morphine or oxycodone
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