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The aim of the present study was to investigate the
2019-12-20

The aim of the present study was to investigate the participation of CRF1 and CRF2 in the alterations of the dorsal and ventral striatal dopamine release and the vertical and horizontal locomotor activity observed in rats following chronic nicotine treatment and consequent acute withdrawal. In this
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Apart from its high affinity
2019-12-19

Apart from its high affinity, the selection of GW2580 as BI-847325 synthesis lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct co
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The pharmacokinetics properties of compound were evaluated i
2019-12-19

The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability
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br Introduction The dorsal periaqueductal gray matter dPAG i
2019-12-19

Introduction The dorsal periaqueductal gray matter (dPAG) is a midbrain site markedly involved in fear/anxiety-evoked responses as well as in nociception (see, for example, Bandler and Carrive, 1988, Deakin and Graeff, 1991, Fardin et al., 1984a, Fardin et al., 1984b, Litvin et al., 2007). Chemic
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Many studies have shown that curcumin
2019-12-19

Many studies have shown that curcumin delays the progression of atherosclerosis in different atherosclerotic animal models [18], [19], [20], [37] and the risk of atherosclerosis in human studies [15], [38], [39]. Curcumin also has many properties that contribute to combat atherosclerosis, such as an
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ketorolac toradol br Results and discussion br Conclusion
2019-12-19

Results and discussion Conclusion Recent studies showed that EGFR signaling is involved in inflammatory response in several inflammatory conditions. The normal inflammatory macrophage ketorolac toradol show EGFR-dependent production of inflammatory mediators. Nevertheless, the development of
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Previous research has suggested that the acetylcholine
2019-12-18

Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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It has previously been established that DDRs play an importa
2019-12-18

It has previously been established that DDRs play an important role in collagen regulation in at least two distinct ways: (1) activation of DDRs by collagen results in up-regulation of the matrix metalloproteinases, which results in cleavage and degradation of the ECM20., 21., [22] and (2) Myosmine
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Ubiquitin activating enzyme activates ubiquitin by
2019-12-18

Ubiquitin-activating enzyme activates ubiquitin by a three-step process with ATP as a cofactor (Chen et al., 2011, Haas and Rose, 1982, Haas et al., 1982). We demonstrated that ATP is required for mRFP-Ub–E1 formation under non-reducing conditions (Fig. 2A). A time course of radioactive ATP producti
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In vitro work by us
2019-12-18

In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan
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A series of monocarboxylated chalcones e g
2019-12-18

A series of monocarboxylated chalcones (e.g. compounds 7 and 8, Fig. 2A) was previously identified as good CysLT1 antagonists [20], and none of them exhibited CysLT2 antagonistic activities (Supplementary Table S1). This study was consistent with reported result that CysLT2 Levodopa australia was no
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br Advantages of modified proteins over unmodified ones
2019-12-18

Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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The following is the supplementary data related to this arti
2019-12-18

The following is the supplementary data related to this article. Funding This work was supported by departmental funding to Prof. Mühl. Funding derived from the State of Hessia to the Institute of General Pharmacology and Toxicology at the pharmazentrum frankfurt (Head: Prof. Josef Pfeilschifter
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br Experimental br Declaration of interest
2019-12-18

Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR caspofungin library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound was modified
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For this reason downstream components of the
2019-12-18

For this reason, downstream components of the inflammatory pathway have been investigated in the search for alternative targets. Targeting such downstream elements might result in safer and more tolerable analgesics. PGE mediates its effects through binding to four G-protein-coupled receptors (EP1-4
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