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br Declaration of interest br
2022-01-07

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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br FAAH mediation of fear
2022-01-07

FAAH mediation of fear and extinction In addition to being a major target and modulator of stress, the BLA is a critical node within the neural circuitry subserving learned fear behaviors. The BLA is activated during the formation, expression, and extinction of conditioned fear memories, and dama
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Acetylation of histones by histone
2022-01-07

Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing Anisomycin receptor structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Recen
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br Conclusion H R H R
2022-01-07

Conclusion H1R, H2R, and H3R mRNAs were expressed in rat OE. Moreover, these three histamine receptors were present in the cytoplasm of ORNs in OE. This is the first report of the expression and localization of histamine receptors in mammalian OE. These findings indicate that histamine may play a
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br Discussion The aim of the present study was
2022-01-07

Discussion The aim of the present study was to extend the list of ASIC ligands and to check if histamine receptors ligands can also affect ASICs. The novel finding is that not only histamine but also thioperamide, 1-metylhistamine and Nα-methylhistamine are active ASIC1a potentiators, while other
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Other N substituted carboxamide oxy pyridine derivatives a
2022-01-07

Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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br Conclusions br Acknowledgements The authors thank Matt JM
2022-01-06

Conclusions Acknowledgements The authors thank Matt JM Wood and colleagues (AstraZeneca, UK) for permission to use logD and protein binding data presented in Sup. Table S2. Introduction The number of people suffering from type 2 diabetes mellitus (T2DM) has escalated worldwide as a consequ
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We recently reported the first cyclopropene analog
2022-01-06

We recently reported the first cyclopropene-analog of the amino Thonzonium Bromide sale neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and cowor
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The third generation cephalosporin antibiotics can
2022-01-06

The third-generation cephalosporin 5-EdU can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when taken orally, CEF must
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About epilepsy no specific seizure type has been
2022-01-06

About epilepsy, no specific seizure type has been identified because GLUT1-DS is associated with a wide range of epilepsies: patients develop seizures in infancy and early childhood, which are, frequently, do not respond to anticonvulsant medication. In infants, seizures are described as brief, subt
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br Introduction HH GLI signaling is one of the
2022-01-06

Introduction HH-GLI signaling is one of the major pathways involved in both normal and neoplastic development [[1], [2], [3], [4]]. Inappropriate activation of this pathway has been linked to cancer, including medulloblastoma, rhabdomyosarcoma, basal cell carcinoma and cancers of the lung, stomac
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In order to facilitate the preparation
2022-01-06

In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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As with the GSIs there are again major concerns that
2022-01-06

As with the GSIs, there are again major concerns that GSM therapy in patients with symptomatic AD is almost certain to fail, unless the compound has additional mechanism of action not linked to Aβ that prove to beneficial [52]. Although Aβ1–42 or other longer Aβ peptides are critical for initiating
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Despite their undisputed importance however FPR receptors ar
2022-01-06

Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis
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Following the discovery of diketo compounds S
2022-01-06

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent nutlin 3 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioas
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