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Fatty acid amide hydrolase FAAH is a membrane bound
2021-12-08
Fatty gamma-Glu-Cys amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion via a
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Nowadays it is accepted that ligands which have been classic
2021-12-07
Nowadays, it is accepted that ligands which have been classically described as inverse agonists, due to their negative efficacy at modulating the G protein pathway, could also display some positive efficacy regarding receptor desensitization, internalization, or even signaling though another pathwa
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br Conclusion The addition of cellulose to
2021-12-07
Conclusion The addition of SAR405838 receptor to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two H-bond
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There are five main research
2021-12-07
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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The first described synthetic FFA active agonist GW phenoxyp
2021-12-07
The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was
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Methyllycaconitine citrate A linker length of and atoms was
2021-12-07
A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and d
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br Animal models of NASH
2021-12-07
Animal models of NASH The human NAS system (see above) is largely reproducible in NAFLD mouse models [37] and, therefore, has been increasingly applied in the preclinical assessment of liver histological responses to test compounds. In general, the NAS system is well suited for this purpose, alth
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To further implicate the role of EAAT in morphine
2021-12-07
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 ciprofloxacin australia was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wil
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In the present study compared to diabetic control rats hepat
2021-12-07
In the present study, compared to diabetic control rats, hepatic glucose-6-phosphatase activity was significantly decreased in both SE and METF treated diabetic animals, with the latter producing greater reduction in glucose-6-phosphatase activity. This observation is consistent with the claim of Ta
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Acknowledgments br Introduction Type diabetes mellitus T DM
2021-12-07
Acknowledgments Introduction Type 2 diabetes mellitus (T2DM) is caused by relative insulin deficiency or insulin resistance in peripheral tissues. The clinical management of T2DM is achieved by controlling blood glucose levels. Current therapies available for treatment of T2DM include biguanides
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Despite the potential promise of both
2021-12-07
Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty Senexin A dervatisation of related regulatory peptides resul
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Receptor interactions and binding mode
2021-12-06
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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Chlorocresol receptor Overall while cART has significantly p
2021-12-06
Overall, while cART has significantly prolonged life and ameliorated HIV-associated disease, HIV infection of the CNS still induces a number of cognitive, behavioral and motor symptoms, along with substantial neuropathology. Data show that the inflammatory processes driving neurological disease pers
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In the CNS histamine is known to regulate
2021-12-06
In the CNS, Guanfacine hydrochloride is known to regulate sleep and wakefulness, learning and memory, feeding, and energy. Here, we address its actions in relation to CNS disorders, and emphasize potential clinical applications of histamine receptor ligands (Table 1). In addition, as the effect of
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Histamine H and H receptors are considered as low
2021-12-06
Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo
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