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br Methods and materials br Results
2022-04-11
Methods and materials Results To examine the fear conditioning effects of the pre-exposure, drug, and sex factors in the total latency time, a 2 × 3 × 2 three-way ANOVA indicated that RGFP966 receptor significant differences occurred in the drug (F2109 = 14.44, p 0.05) and pre-exposure × sex
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AZD2932 receptor k j and d were
2022-04-11
15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil
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Despite potent biological actions the native hormone
2022-04-09
Despite potent biological actions, the native hormone undergoes degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV) [17] and is rapidly cleared from the bloodstream by renal filtration [18]. One such approach to prolong the biological half-life of GIP is through conjugation with a polyethylene
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By association a possible mechanism which may
2022-04-09
By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et
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Seizures in turn selectively modulate the expression of GalR
2022-04-09
Seizures, in turn, selectively modulate the apexbt kinase inhibitor of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could
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Retinal GAL receptor distribution suggests an intrinsic neur
2022-04-09
Retinal GAL receptor distribution suggests an intrinsic neuronal control since retina lacks an autonomic innervation, and a signal modulation seems most likely here, acting via GALR1 while GALR2 and GALR3 seem to play a rather minor role in this signal transduction. While sources acting on these ret
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The first FPR ligand described is the fMLF
2022-04-09
The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o
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We have presented evidence that
2022-04-09
We have presented evidence that only muscle FBPase is detectable within HL-1 cells. This is consistent with past findings of the Eschrich's group, which showed that in rat heart Meleagrin expression of FBPase is almost exclusively limited to the muscle isozyme [3]. Results of our preliminary exper
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Sumoylation of transcription factors has been
2022-04-09
Sumoylation of transcription factors has been generally linked to transcriptional repression and, in a few cases, to transcriptional activation [60] Accumulating evidence implies that corepressor complex subunits, including CoREST, CtBP, Daxx, NCoR1, SMRT and histone deacetylase complexes (HDACs), p
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Adipocytes play diverse roles in
2022-04-09
Adipocytes play diverse roles in energy homeostasis by controlling energy consumption [8] and function as a source of proteins and cytokines, which mediate numerous physiological functions [9]. Excessive accumulation of adipocytes, as well as an increase in either their size or number, causes obesit
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Despite the two models for the HIV IN aptamer
2022-04-09
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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Noticeably aminopyrimidine analogs are the most
2022-04-09
Noticeably, aminopyrimidine analogs are the most widely published H4R antagonists and it was Bayer who first disclosed two series of 2-aminopyrimidine compounds possessing significant H4R functional activity. Subsequently, further 2-aminopyrimidine H4R antagonists were published by Pfizer (ZPL-38937
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Progesterone Although histamine can induce both proliferatio
2022-04-09
Although histamine can induce both proliferation and differentiation in vitro (Molina-Hernandez and Velasco, 2008), the promotion of neurogenesis conferred by H3R antagonism here does not seem to be caused by either the proliferation or the reduction of apoptosis of NSCs (Figure S3). Furthermore, H3
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br Conclusions In summary our results demonstrate that in sh
2022-04-09
Conclusions In summary, our results demonstrate that in short term effect, TBT induced concentration-dependent vasorelaxation of HUA rings. Regarding the long term effects, exposure to a concentration of 100 μM TBT the human umbilical NMS-E973 have a dual effect, and a decrease of the 5-HT2A exp
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Nowadays it is accepted that ligands which
2022-04-09
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 pathway
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