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br Medium and long chain fatty acid receptors br
2022-04-02

Medium- and long-chain fatty rotenone receptors Clinical studies of ω3 fatty acids Clinical studies have established that dietary intake of ω3 fatty acids should be around 4g/day for treating very high triglyceride levels (≥5.7mmol/L) [36]. Low-dose supplementation with EPA + DHA (400mg/day)
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There is no doubt that GPR
2022-04-02

There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago
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Introduction l Glutamate is a major excitatory neurotransmit
2022-04-01

Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is
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We also demonstrated that inhibition of NAAG
2022-04-01

We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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br Methods GLUT DS was diagnosed
2022-04-01

Methods GLUT1DS was diagnosed either when analysis of the SLC2A1 gene showed a pathogenic mutation and/or when cerebrospinal fluid (CSF) analysis met the criteria for GLUT1DS: a CSF ZD 7288 synthesis below the 10th percentile, a cerebrospinal fluid (CSF) to blood ratio below the 25th percentile a
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leukotriene receptor agonist A significant contribution to t
2022-04-01

A significant contribution to the discovery of novel Hh inhibitors is given by natural compounds [11,17,22,31,32]. The first Hh inhibitor ever discovered has been Cyclopamine, a steroidal alkaloid isolated from plants of the Veratrum species [13,33]. Subsequently, many natural compounds belonging to
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It is widely acknowledged that a significant gap
2022-04-01

It is widely acknowledged that a significant gap exists between the increasingly detailed knowledge of subcellular mechanisms and the ability to control large-scale anatomy. Radical advances in regenerative medicine require approaches aimed at taming the fundamental complexity of cellular regulation
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More polar substituents introduced on the position of
2022-04-01

More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in mic
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To improve the preferential GalR binding we
2022-04-01

To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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Further insight in how exactly galanin might inhibit seizure
2022-04-01

Further insight in how exactly galanin might inhibit seizures was obtained from galanin transgenic mice. It occurred that the altered susceptibility to seizures was in direct correlation with glutamate release from hippocampal slices obtained from these animals (Fig. 2(b)). While no differences were
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br Material and methods br Results br Discussion Propofol
2022-04-01

Material and methods Results Discussion Propofol is commonly used in operation rooms or intensive care units (ICUs) for critically ill patients. Various clinical trials have demonstrated that the antioxidant, anti-inflammatory, and free-radical-scavenging properties of propofol can provide
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On the contrary the benzhydrol series
2022-04-01

On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the Atropine tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the unsubs
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Several observations about structure activity
2022-04-01

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic TASIN-1 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of
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Despite the two models for the
2022-04-01

Despite the two models for the HIV-1 IN-aptamer complexes appeared to be comparable, disintegration assays revealed that 93-del inhibited C– or N-terminally truncated enzyme at the same extent, [18] whereas, T30695 required N-terminal domain (NTD) of the enzyme to exert its integrase inhibitory acti
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AZ505 ditrifluoroacetate Hippo pathway proteins could synerg
2022-03-31

Hippo pathway proteins could synergistically regulate germ cell development with some specific receptors. Kassab et al. [27] found that epidermal growth factor (EGF) receptor was localized in testicular germ AZ505 ditrifluoroacetate and played important roles in bovine spermatogenesis. Likewise, ins
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