• br Histamine H R The cloning

  2022-06-15

  

  Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other K-Ras(G12C) inhibitor 12 receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et

• ANT located in the IMM mediates

  2022-06-15

  

  ANT, located in the IMM, mediates the exchange of ATP/ADP between the mitochondrial matrix and the intermembrane space (IMS) (Brand et al., 2005; Palmieri and Pierri, 2010). Of the 4 known isoforms, ANT1 is the dominant isoform in the heart (Palmieri and Pierri, 2010). Under physiological conditions

• In conclusion while class I HDAC inhibitors

  2022-06-15

  

  In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides

• Although it has been observed in numerous

  2022-06-15

  

  Although it has been observed in numerous studies and by many investigators that intraplatelet cGMP elevation results in platelet inhibition, there are a few papers which proposed a platelet stimulatory role for cGMP when elevated in response to NO donors or PDE5 inhibitors in mouse and human platel

• br Conclusion The development discovery of compounds targeti

  2022-06-15

  

  Conclusion The development/discovery of compounds targeting small GTPases is challenging [43,44]. Our data point to RBC8 being efficient and potent as a Ral inhibitor in human and mouse platelets, but that it exhibits some activity beyond just Rals, particularly in mouse platelets. It is however

• The first described synthetic FFA active agonist GW phenoxyp

  2022-06-14

  

  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

• The differential tissue and ligand dependent

  2022-06-14

  

  The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va

• br Materials and methods br Results br Discussion In the

  2022-06-14

  

  Materials and methods Results Discussion In the CNS, GLP-1R is associated with G-protein signal transduction pathways, which can activate adenylyl cyclase and protein kinase A by cyclic adenosine monophosphate, and mediates neuronal activities implicated in various pathophysiological change

• As ghrelin effects are suspected to be mediated

  2022-06-14

  

  As ghrelin effects are suspected to be mediated by a heterogeneous population of G-protein-coupled-receptors [2], [21], other so far unknown subtypes of ghrelin receptors differing from the classical GHSR-1a may additionally exist that might also mediate ghrelin effects on the heart. Thus, the real

• GYY 4137 morpholine salt Another key component of proper

  2022-06-14

  

  Another key component of proper DA cell physiology is the basal firing activity of SN DA neurons, which maintains extracellular levels of dopamine in the dorsal striatum that are essential for voluntary movement [106]. Changes in SN DA neuron activity directly impacts the amount of dopamine released

• A mutation in stearoyl coenzyme A desaturase gene

  2022-06-14

  

  A mutation in stearoyl coenzyme A desaturase 1 gene was reported to reduce sebum production and monounsaturated fatty acids (MUFA) synthesis in mice, which was accompanied with impaired clearance of gram-positive bacteria-induced skin infection (Georgel et al., 2005). Interestingly, gram-positive ba

• The receptor binding assay used in our previous study

  2022-06-14

  

  The receptor binding assay used in our previous study demonstrated that propofol competitively binds to FPR1, thus blocking the downstream signal transduction of FPR1 and inhibiting neutrophil immune activities [8]. In this study, we assessed the pharmacological action of fMMYALF in the presence of

• br Results The RAS MEK ERK pathway is a potential

  2022-06-14

  

  Results The RAS/MEK/ERK pathway is a potential target of FGFR signaling. Indicative for its activation is the presence of double phosphorylated (activated) ERK (dpERK), which is generated in a series of phosphorylation events downstream of FGFR (op. cit. (Lemmon and Schlessinger, 2010)). Followin

• Methods Very briefly PLA polymeric nanoparticles as well as

  2022-06-14

  

  Methods Very briefly: PLA polymeric nanoparticles as well as liposomes were synthesized and loaded with three different FGFR inhibitors. The encapsulation efficiency, average size, PDI, zeta potential, stability and release kinetics were investigated. The most promising formulations were biological

• The first suggestion that histamine

  2022-06-13

  

  The first suggestion that histamine may play a role in memory consolidation was from Almeida and Izquierdo (de Almeida & Izquierdo, 1986) who showed that the immediate posttraining intracerebroventricular (i.c.v.) administration of 1–10ng of the drug were found to enhance the retention of one-trial

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