• br Acknowledgments R Dalmann has obtained a bourse

  2022-08-02

  

  Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport

• br Materials and methods br Results

  2022-08-02

  

  Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka

• It is an exciting time for translational histamine research

  2022-08-01

  

  It is an exciting time for translational histamine research, since preclinical studies show potential value for histamine receptor ligands. As reviewed above, there are several concerns for future studies of histamine and its role in the CNS. 1) Because of the availability of HDC-Cre mice (Williams

• br Dual acting HR antagonists While the present medicinal

  2022-08-01

  

  Dual-acting HR antagonists While the present medicinal chemistry efforts are mainly focused on selective ligands targeting GPCRs, and particularly on H1R, H3R and H4R selective antagonists/agonists, there were and, also, still are several efforts to develop dual acting H1R/H2R, H1R/H3R and H3R/H4

• Several named antagonist ligands have

  2022-08-01

  

  Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l

• Sometime ago we have described diamino triazines as histamin

  2022-08-01

  

  Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by Trovafloxacin mesylate and zymosan. In this work we descr

• One of the possibilities of HO targeting is gene therapy

  2022-07-30

  

  One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing Argatroban but also have very limit

• In our previous study we designed and synthesized compounds

  2022-07-30

  

  In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic AZD6482 (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro antitumor p

• In our previous study we designed and synthesized compounds

  2022-07-30

  

  In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic AZD6482 (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro antitumor p

• br Conclusion B esterases and reproductive

  2022-07-30

  

  Conclusion B-esterases and reproductive parameters can be used as effect biomarkers of the aquatic contamination with chlorpyrifos. In P. corneus exposed for 14 days to the insecticide, the carboxylesterases determined with p-NFB proved to be the most sensitive biomarker. However, exposure to env

• br Materials and methods br Results br Discussion D abbrevia

  2022-07-30

  

  Materials and methods Results Discussion D. abbreviatus larvae are voracious feeders, and the nutrients consumed as part of their diet are broken by gut proteases and utilized for growth and development. Since proteases play an important role in larval and adult food digestion, it is import

• br Intracellular trafficking with concurrent signaling of NP

  2022-07-30

  

  Intracellular trafficking with concurrent signaling of NPRA Our recent studies have shown internalization and concurrent signaling of NPRA in subcellular compartments; this had not been previously demonstrated [26,42]. Preparation of the enhanced GFP (eGFP)-tagged NPRA (eGFP-NPRA) construct has g

• Since KYNA concentrations are increased by aerobic exercise

  2022-07-29

  

  Since KYNA concentrations are increased by aerobic exercise training, we have investigated if it plays a role in peripheral tissue metabolism. Here we show that KYNA regulates adipose tissue energy homeostasis through activation of Gpr35. Activation of this network stimulates the expression of lipid

• PU-WS13 br Gastrointestinal peptides and intestinal health G

  2022-07-29

  

  Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)

• br TGR Agonists br FXR TGR

  2022-07-29

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

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