• Several studies have found that GPR possesses a

  2022-01-05

  

  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 7ACC2 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimona

• In vitro studies have shown that some antidepressant

  2022-01-05

  

  In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found t

• (±)-Epibatidine br Experimental br Acknowledgments This

  2022-01-05

  

  Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t

• Chitosan CS a deacetylated derivative of

  2022-01-05

  

  Chitosan (CS), a deacetylated derivative of chitin, was chosen in this study due to its unique biological characteristics including biodegradability, biocompatibility, non-toxicity, and antimicrobial properties (Klossner, Queen, Coughlin, & Krause, 2008; Kong, Chen, Xing, & Park, 2010; Ravi Kumar, 2

• Another small compound targeting IBAT has been evaluated

  2022-01-05

  

  Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause

• br Material and methods br Results

  2022-01-05

  

  Material and methods Results Discussion Propofol is commonly used in operation rooms or intensive care units (ICUs) for critically ill patients. Various clinical trials have demonstrated that the antioxidant, anti-inflammatory, and free-radical-scavenging properties of propofol can provide

• Corresponding to the different insulinotropic signaling the

  2022-01-05

  

  Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct 961 on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonists [8]

• br Ferroptosis modulators With the recognition that the

  2022-01-05

  

  Ferroptosis modulators With the recognition that the small molecule erastin targets system xc- and thereby specifically triggers this form of death and that ferrostatin-1 prevents erastin-induced ferroptosis [2], it has become evident that ferroptosis is a druggable pathway with a number of tract

• l-name mg Contrary to the transient nature of signal transmi

  2022-01-05

  

  Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system

• Hyperactivation of Notch pathway can give rise to

  2022-01-05

  

  Hyperactivation of Notch1 pathway can give rise to transformation into T-ALL in murine models. In more than 50% of acute T-cell lymphoblastic leukemias oncogenic activating mutations of Notch1 have been detected and inactivation of Notch1 signaling impairs leukemia cell proliferation and promotes ap

• Increasing trans epithelial transport efficiency is another

  2022-01-05

  

  Increasing trans-epithelial transport efficiency is another area where different strategies are being developed for overcoming transcytosis. Enhancing the affinity for the basal membrane and weakening apical exocytosis through the optimisation of surface hydrophobicity have been demonstrated [79]. S

• The biological activity at GPR a of each of the

  2022-01-04

  

  The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu

• The PK profile and tissue distribution

  2022-01-04

  

  The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an

• Prion diseases are transmissible and result in

  2022-01-04

  

  Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in Calcium Gluceptate lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, c

• br Methods br Results It is

  2022-01-04

  

  Methods Results It is well known that during the onset of vasoconstriction there is an increase in intracellular Ca2+ which activates myosin light-chain kinase followed by cycling of actin-myosin cross-bridges in VSMCs. Recently, it has been recognized that N-Nonyldeoxynojirimycin polymerizat

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