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Compounds and were synthesized according to The synthesis
2022-08-04
Compounds –, , and were synthesized according to . The synthesis of compounds – commences with C-acylation of 3,4-dibromothiophene to the form ketone , the ring closure to form the ester , Hiyama cross-coupling or Suzki cross-coupling to produce , or to , respectively. Compound was produced from ket
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Similar to GPR A activation
2022-08-04
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic Phosphoramidon Disodium Salt mg receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008,
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Introduction Histamine was generally accepted as a neurotran
2022-08-03
Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activiti
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The eradication of agonist activity in compound was also con
2022-08-03
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary Azaserine sale as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagon
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The ultimate success of multimodal probe in
2022-08-03
The ultimate success of multimodal probe in the inflammation imaging will be dependent on simplicity in synthesis (combining various modules without protection/deprotection), ease of optimization of pharmacological properties (linker group with tunable PEG moiety), co-registration of macroscopic and
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The root of Danshen has
2022-08-03
The root of (Danshen) has been widely used as traditional Chinese medicine for many years and shown to exhibit significant pharmacological activities for a variety of human diseases including cancers. Tanshinones, the major active components, belong to a group of an abietane-type diterpenes containi
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br Author contributions br Acknowledgements The work was sup
2022-08-03
Author contributions Acknowledgements The work was supported in part by Natural Science Foundation of China (31601995, 31501028) and an internal research grant of Jianghan University (14042). The authors thank HY of Jingchu University of technology for revising the manuscript. Introduction
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br Acknowledgements This work was financially
2022-08-03
Acknowledgements This work was financially supported by the National Natural Science Foundation of China (Grant No. 81803033) and the “Double First-Class” University project (CPU2018GF02). Introduction Atrial fibrillation (AF) is the most common progressive cardiac rhythm disorder. Studies ha
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Any brain damage including that caused by
2022-08-02
Any 8-Bromo-cAMP, sodium salt damage, including that caused by β-amyloid, triggers activation of microglia, the resident immune cells of the CNS. These cells cluster around amyloid plaques, in which they extend cytoplasmic processes (Combs, 2009). The significance of this response is controversial,
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Introduction Substantial body of evidence supports
2022-08-02
Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that
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In summary we have developed an efficient synthetic route to
2022-08-02
In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ
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br Materials and methods br Results br Discussion In
2022-08-02
Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the Caspase-10/a, human recombinant
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Na K ATPase adenosine triphosphate
2022-08-02
Na+/K+-ATPase, Shikonin and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increased as from 24 h.
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br Materials and methods br Results Aberrant
2022-08-02
Materials and methods Results Aberrant Aβ has been suggested to be an initiating factor for glutamate excitotoxicity in AD pathology. To investigate whether Aβ1-42 alters glutamate uptake in astrocytes, neurons, and astrocyte-neuron co-cultures, we used synthetic Aβ1-42 peptide. Aβ1-42 has fas
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Transmembrane AMPA receptor regulatory proteins TARPs are a
2022-08-02
Transmembrane AMPA receptor regulatory proteins (TARPs) are a relatively newly discovered protein family. Prototypic TARP, stargazin, was found by a spontaneous mutation in ataxic stargazer mouse line as a homologous protein to γ1 calcium channel subunit (Letts et al., 1998). The role of stargazin i
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