• GPR agonistic activity was evaluated for the human GPR recep

  2022-05-26

  

  GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin

• It is important to clarify whether

  2022-05-26

  

  It is important to clarify whether the decrease in USV after administration was secondary to the central depressant actions of the test compounds. Several reports have addressed the possibility that central depressant actions such as motor incoordination or changes in body temperature might affect U

• caudatin receptor Although glycine receptors predominate in

  2022-05-26

  

  Although glycine receptors predominate in the brain stem and spinal cord, they are also expressed in higher brain regions such as the nucleus accumbens, frontal cortex, and hippocampus (Jonsson et al., 2012, Jonsson et al., 2009, Molander and Söderpalm, 2005b). A variety of drugs of abuse, including

• Imipramine hydrochloride The need for an inflammatory risk p

  2022-05-26

  

  The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab

• All models used here rely on

  2022-05-26

  

  All models used here rely on WT FGFR3, which is activated by exogenous FGF ligand to alter chondrocyte proliferation and differentiation. This approach toward modeling the aberrant FGFR signaling in cartilage differs from the actual situation in ACH or TD, where the chondrocytes are exposed to long-

• Current studies have identified five orphan G protein couple

  2022-05-26

  

  Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs

• To explain the corporate debt maturity following Brockman

  2022-05-26

  

  To explain the corporate debt maturity, following Brockman et al. (2010), the time-varying control variables we include are: firm size (LSIZE), the square of firm size (LSIZE2), leverage (LEVERAGE), asset maturity (ASSET_MAT), managerial ownership (OWN), market-to-book ratio (MB), term structure of

• br Materials and methods br Results

  2022-05-26

  

  Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str

• br Introduction Soluble guanylyl cyclase GC maintains vascul

  2022-05-25

  

  Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.

• We found that activator drugs decrease NOsGC protein levels

  2022-05-25

  

  We found that activator drugs decrease NOsGC protein levels in Sf9 cells. This decrease in protein levels is more pronounced for BAY 60–2770 compared to cinaciguat, and more obvious for α1/β1 compared to α2/β1 (see Fig. 2). This led us to hypothesize that the reduction in protein level correlates wi

• The involvement of prostaglandins on

  2022-05-25

  

  The involvement of prostaglandins on the effects induced by 1-nitro-2-phenylethane is similarly unlikely because vasorelaxation was not changed by indomethacin [20]. The inhibition of adenylyl cyclase with MDL-12330A [21] or cAMP-dependent protein kinase A with KT-5720 [22] also did not interfere wi

• br Acknowledgements br Introduction The glutathione S transf

  2022-05-25

  

  Acknowledgements Introduction The glutathione S-transferase (GST, EC 2.5.1.18) family of multifunctional enzymes plays a particularly important role in cellular detoxification [1]. Over-expression of the GSTP1 isoform characterizes many human tumor cell lines derived from stomach, brain and co

• In summary we have successfully identified a series of poten

  2022-05-25

  

  In summary, we have successfully identified a series of potent and selective GSNOR inhibitors having imidazole and tetrazole functional groups in both end of the core structure and many compounds have been identified with IC: Introduction Peppers (Capsicum annuum L.), tomatoes and potatoes, belon

• Using RT PCR we demonstrated the expression of GPR

  2022-05-25

  

  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

• Typically upon chronic agonist exposure GPCRs undergo

  2022-05-25

  

  Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have

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