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Although drug monitoring is not usually requested there
2022-03-30

Although drug monitoring is not usually requested, there are some cases where measurement of DOACs in OG-L002 is useful, and of special help for managing patients at risk. These cases include the control of adherence to a therapeutic protocol, surveillance of drug accumulation risk in long term tre
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Although histamine can induce both proliferation and differe
2022-03-30

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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SCH is a H R receptor antagonist introduced by
2022-03-30

SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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GSK has also been used
2022-03-30

GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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br Acknowledgments br Introduction Lung
2022-03-30

Acknowledgments Introduction Lung cancer is a common but extremely perilous cancer, with approximately 733,000 new incidences reported annually in China [1]. Lung cancer ranks highest in the causes of tumor-related mortality, accounting for approximately one quarter of all cancer deaths [2]. N
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Tarafenacin br Materials and methods br Results br
2022-03-30

Materials and methods Results Discussion Both EMT of the tubular epithelial Tarafenacin and the activation of fibroblasts are critical factors in the pathogenesis and progression of renal interstitial fibrosis. Accumulating evidence implicates EMT in the onset and pathogenesis of renal int
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Considering that TGF plays a
2022-03-30

Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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There are five subfamilies of P type ATPases I
2022-03-30

There are five subfamilies of P-type ATPases (I-V), which transport metal ions or phospholipids across membranes (Palmgren and Nissen, 2011). Although our studies indicate that the P-type ATPase domain is important for function, how it contributes to cGMP production is currently unknown. The P-type
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br Acknowledgments We thank Dr Kathleen Sullivan
2022-03-29

Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 UNC2025 mg expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. Andrew
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Using RT PCR we demonstrated the expression of
2022-03-29

Using RT-PCR we demonstrated the expression of GPR55 receptor mRNA in the ileum and colon of mice, which is in good agreement with previous reports (Lin et al., 2011). The quantitative analysis showed the abundance of GPR55 mRNA in the mucosa of the ileum and colon. In contrast, in LMMP preparations
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Also the decrease in adipocyte
2022-03-29

Also, the decrease in adipocyte cAMP levels seen after an acute glucose challenge in wild-type mice was strongly reduced in mice lacking GPR81, indicating that the activation of PDE3B alone was not sufficient to mediate the effect of insulin on cAMP levels and lipolytic activity. The fact that insul
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With an ever increasing incidence rate of
2022-03-29

With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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To shed more light on the
2022-03-29

To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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p38 inhibitors Hesperidin is an abundant and inexpensive
2022-03-29

Hesperidin is an abundant and inexpensive plant flavonoid, largely derived from citrus species including sweet orange and lemon. Hesperetin (Hst) is the aglycone of hesperidin. Hesperidin and hesperetin have been reported to show a battery of pharmacological properties, including anti-hyperlipidemic
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AFB Fapy dG has been long recognized as a substrate
2022-03-29

AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by neuraminidase inhibitor excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-
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