• Andexanet alfa works as a decoy for the FXa

  2022-01-19

  

  Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic

• The FAAH inhibitor activity of the ethoxycarbonyl phenyl H

  2022-01-19

  

  The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound

• While histone modifications can alter inter nucleosomal inte

  2022-01-18

  

  While histone modifications can alter inter-nucleosomal interactions that govern the compaction state of a chromatin fiber (Francis et al., 2004, Kalashnikova et al., 2013, Lu et al., 2008), the potential impact of histone modifications on higher-order chromosome organization beyond chromatin-fiber 

• The therapeutic potential of acetate has been advocated by

  2022-01-18

  

  The therapeutic potential of acetate has been advocated by research on neurodegenerative disorders such as Canavan's disease (Arun et al., 2010, Mathew et al., 2005), where oral acetate improved motor function in a genetic model of the disorder, and in studies of behavioural phenotypes associated wi

• br STAR Methods br Acknowledgments We thank Prof Y

  2022-01-18

  

  STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a

• 8-Azido-ATP The relaxant response to carperitide was influen

  2022-01-18

  

  The relaxant response to carperitide was influenced neither by the removal of the endothelium nor by treatment with the nitric oxide synthase inhibitor or nitric oxide scavenger. This result was to be expected as previous studies showing that the vasodilator action of atrial natriuretic peptide is

• Distribution of Iodine labeled ANP I

  2022-01-18

  

  Distribution of 125Iodine-labeled-ANP (125I-ANP) radioactivity on the cell surface, in the intracellular compartments, and in culture medium established a dynamic equilibrium of receptor-mediated 125I-ANP uptake, degradation, and release outside of N6-Methyl-dATP (Fig. 2). A major proportion of int

• The endocannabinoid system ECS consists

  2022-01-18

  

  The endocannabinoid system (ECS) consists of cannabinoid (CB)1 and CB2 receptors, their endogenous ligands anandamide and 2-arachidonylglycerol, and the synthesizing and degrading enzymes for these ligands. Cannabinoids and the ECS are involved in the regulation of GI motility in physiological and p

• Several studies have found that GPR possesses

  2022-01-18

  

  Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected 487 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimonaba

• Little is known about the role of GPR

  2022-01-18

  

  Little is known about the role of GPR35 in physiology and pathology. Using GPR35 knockout and wild-type mice showed that GPR35 activation by KYNA improves energy metabolism and inflammation, while demonstrated that GPR35 plays an important role in the development of angiotensin II-induced hyperten

• Finally we investigated if calpain truncation affects GlyT t

  2022-01-18

  

  Finally, we investigated if calpain truncation affects GlyT1 turnover and trafficking. To simulate calpain cleavage at the T602/T603 and G626/S627 sites we constructed GlyT1 transporters missing the last 12 and 36 amino acids. Since the 36 amino GSK503 mg truncation also removes all C-terminal anti

• Variants of NEIL were also analysed in

  2022-01-18

  

  Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo

• Ning et al showed that LPC appeared

  2022-01-18

  

  Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p

• ICH induced striatal lesion produced a reduction of

  2022-01-18

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino sc9 synthesis transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischem

• br The hippocampus and spatial memory Numerous lines of

  2022-01-18

  

  The hippocampus and spatial memory Numerous lines of evidence have implicated the rodent hippocampus in spatial forms of learning and memory (O’Keefe and Nadel, 1978). For example, hippocampal lesions produce robust and reliable deficits on spatial memory tasks such as the Morris watermaze in bot

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