• br Methods br Results br Discussion Our results show that

  2021-09-16

  

  Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of

• For some agonists these stable GPR responses were

  2021-09-16

  

  For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer

• As part of our discovery efforts searching for

  2021-09-16

  

  As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragmen

• For a long time the mechanism for the TG

  2021-09-16

  

  For a long time, the mechanism for the TG-lowering effect of nicotinic 71 5 has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested the involvement of

• In conclusion we demonstrated that

  2021-09-16

  

  In conclusion, we demonstrated that extrasynaptic glutamate could in situ affect the AA metabolism via brain CYPs. CYP1B1 and CYP2U1 genes in the astrocytes are the downstream genes of CREB, and the up-regulation of CYP1B1 and CYP2U1 expression by glutamate was due to the increases in phosphorylated

• br Acknowledgements Supported by the grant from National Nat

  2021-09-16

  

  Acknowledgements Supported by the grant from National Natural Science Funds of China (81371262). I would like to express my heartfelt gratitude to Professor Yonghua Zhu, who help language editing. Introduction Glucocorticoids are steroid hormones secreted from the adrenal glands in response t

• br Glucocorticosteroid receptor structure and function

  2021-09-16

  

  Glucocorticosteroid receptor structure and function The gene encoding for the human GR is composed of 9 exons (Oakley and Cidlowski, 2011) and the translated protein is described as having 4 functional regions. The protein contains a highly conserved central DNA-binding domain (DBD) or C-domain,

• The biological actions of ghrelin are mainly due to

  2021-09-16

  

  The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept

• Analysis of published albumin X

  2021-09-15

  

  Analysis of published albumin X-ray structures had suggested that an allosteric link may exist, but could not establish whether Zn2+ prevented FFA binding or vice versa. This question was answered through competition experiments monitored by isothermal titration calorimetry (ITC; Fig. 3) for BSA [55

• ml calculator Brain derived neurotrophic factor BDNF is the

  2021-09-15

  

  Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of

• FXa is a vitamin K

  2021-09-15

  

  FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 CX-6258 and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102  exhibits the trypsin-like β-barrel structure [12]. The active

• Methods br Results br Discussion

  2021-09-15

  

  Methods Results Discussion SV exocytosis from excitatory boutons is more sensitive to inhibition by isoflurane than exocytosis from inhibitory boutons,4, 31 but the mechanism(s) of this synaptic selectivity is unknown. Although P/Q-type VGCCs contributed quantitatively more to SV exocytosis t

• br Introduction Stroke is the second cause of

  2021-09-15

  

  Introduction Stroke is the second cause of death worldwide and the first cause of acquired motor disability in adults [1], [2]. In sub-Saharan Africa, stroke is the first cause of admission in neurology departments [3]. In Cameroon, the in-hospital mortality of stroke is estimated at 26.8% [4]. A

• br Introduction Ovarian cancer patients have the highest mor

  2021-09-15

  

  Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is cancer 46619 with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone methylation in carc

• The finding of histamine action

  2021-09-15

  

  The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is

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