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In the current study cocaine
2019-12-03

In the current study, cocaine did not significantly increase negative subjective effects and nepicastat did not increase these responses. This outcome is somewhat surprising given that the most commonly reported effect to date has been to increase the aversive properties of cocaine such as anxiety,
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In summary we hypothesize that targeting the A R D
2019-12-03

In summary, we hypothesize that targeting the A1R–D1R heterotetramer with heteromer-selective drugs might improve safety and efficacy of the pharmacological therapy for RLS and other motor diseases, resulting in fewer side effects than classical drugs developed for targeting monomeric A1R or D1R.
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Cdc which is involved in filopodium formation
2019-12-03

Cdc42, which is involved in filopodium formation, and Rac1, which is involved in lamellipodium formation, engage in cross-talk with one another [25,26,30,31]. In general, filopodium formation precedes lamellipodium formation, and filopodium formation (Cdc42 activity) suppresses lamellipodium formati
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Substitutions on the benzene ring of the phenyl acetic acid
2019-12-03

Substitutions on the benzene ring of the phenyl acetic SR 11302 moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryloxy g
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Although enantioselective accumulation of metalaxyl in
2019-12-02

Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms
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The activity of chromenones bearing heteroaryl groups at the
2019-12-02

The activity of chromenones bearing heteroaryl groups at the 8-position is summarised in . Replacement of the 8-phenyl substituent of by a thiophen-2-yl group ( and ) did not improve DNA-PK inhibitory activity, although the 4-phenylthiophen-2-yl derivative (), together with the bithiophene analogue
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In Senegal malaria remains a formidable public health issue
2019-12-02

In Senegal, malaria remains a formidable public health issue, causing significant morbidity and mortality in infants and pregnant women (WHO Malaria Report, 2012). In the absence of an effective vaccine, the National Malaria Control Program has followed WHO recommendations for IPTp-SP since 2003. Th
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Growing evidence has shown that ANS
2019-12-02

Growing evidence has shown that ANS dysregulation, indexed by heart rate variability (HRV), plays a critical role in the pathogenesis of anxiety (Minassian et al., 2014, 2015). Indeed, we have previously reported that patients with GAD are associated with reduced resting parasympathetical (vagal) co
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A more refined picture of cholinesterase activity patterns m
2019-12-02

A more refined picture of cholinesterase activity patterns may be obtained by measuring ChE activity of the same sample before and after addition of certain cholinesterase inhibitors, with differential specificity for different components of total ChE activity, such as BW284c51 (BW1,5-bis-(4-allyldi
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br Roles for intracellular chloride channels br Specific chl
2019-12-02

Roles for intracellular chloride channels Specific chloride channel proteins in intracellular membranes Concluding remarks Introduction The sulfonylurea derivative glybenclamide (GLYB) is used as oral hypoglycemic agent to treat non-insulin dependent diabetes mellitus [1], [2]. The antid
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The authors then showed that Spt
2019-12-02

The authors then showed that Spt6 interacts directly with the PRC2 subunit Suz12. This interaction occurs in solution but not on chromatin, suggesting that Spt6 may prevent PRC2 recruitment by binding to Suz12. They then mapped the domains in both Spt6 and Suz12 that are involved in this interaction
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Despite many studies having demonstrated the importance
2019-12-02

Despite many studies having demonstrated the importance of connexin43 (Cx43), the most abundant connexin in bone cells, for bone development and turnover during the last decade [27], little is currently known about GJIC and Cx43 in primary bone tumors. In this report, we analyzed the specific role o
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2019-11-30

Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase Tubastatin A HCl [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour a
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br Financial Support We would like to acknowledge
2019-11-30

Financial Support We would like to acknowledge financial support by the National Natural Science Foundation of China (grant numbers 81672778 and 81372165) and Natural Science Foundation of Beijing Municipality (grant number 5142009). Acknowledgements Introduction The process of spermatogen
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Previously we have shown that complexes of
2019-11-30

Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabil
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