• The excellent potencies selectivities and improved PK associ

  2024-12-25

  

  The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This

• br ABCA is a sterol responsive gene The

  2024-12-25

  

  ABCA2 is a sterol-responsive gene The first evidence to demonstrate that ABCA2 expression responded to sterol loading was provided in an experiment involving monocyte to macrophage differentiation in vitro. Upon sterol loading with enzymatically degraded LDL (eLDL), ABCA2 expression increased onl

• Enzyme inhibitor In earlier experiments on snails a behavior

  2024-12-25

  

  In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni

• Adenosine receptors are proposed to play proangiogenic role

  2024-12-25

  

  Adenosine receptors are proposed to play proangiogenic role in vascular and immune HL-60 leukemia cells within microenvironment of hypoxic tissues to maintain tissue oxygenation in chronic ischemic condition [9]. Adenosine also stimulates the production of angiopoetin-1, VEGF and Interleukin-6 (IL6

• br Conclusions The present data suggest that homeostatic

  2024-12-25

  

  Conclusions The present data suggest that homeostatic balance of the cortical/hippocampal adenosinergic tone is necessary for normal working memory function and any deviation appears to impair performance – either as a consequence of A2AR under-activation when adenosine levels are reduced or due

• In the present study the alternative splicing of several nAC

  2024-12-25

  

  In the present study, the alternative splicing of several nAChR subunits was identified in the oriental migratory locust (Locusta migratoria manilensis Meyen), a serious worldwide pest to agricultural production and also a model insect species [5]. Several α subunits were tried to co-express with ra

• Taken together our results indicated that

  2024-12-25

  

  Taken together, our results indicated that 5-LOX can be induced in mice by MPTP injection, and the 5-LOX inhibitor MK-886 reduced the death of dopaminergic neurons. MK-886 also reduced the LTB4 SR 2211 induced by MPTP. The development of the novel 5-LOX or FLAP inhibitors may provide a new therapeu

• Additionally regulation of GPCR heteromerization by specific

  2024-12-25

  

  Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut

• Consistent with the observation that mutations in

  2024-12-25

  

  Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t

• Because the V ATPase inhibitors that

  2024-12-25

  

  Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra

• neuropeptides The LOX hydroxide metabolites are converted to

  2024-12-24

  

  The 15-LOX hydroxide metabolites are converted to secondary lipid mediators such as lipoxin A4 from 15-HETE and protectin D1/resolvin D1 from 17-HDoHE [45] (Fig. S3). Importantly, all of these secondary lipid mediators have anti-inflammatory and pro-resolving properties [46], [47], [48]. Lipoxin A4

• The compounds containing beryllium act as

  2024-12-24

  

  The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be Pituitary gland stimulator []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely st

• br Author contributions br Conflicts of interest The

  2024-12-24

  

  Author contributions Conflicts of interest The authors declare no competing financial interests. Acknowledgement This work was supported by grants from the Deutsche Forschungsgemeinschaft (Sonderforschungsbereich/Transregio 166–Project C1 and grant CA 1014/1-1 to D.C.) and the IZKF Würzbur

• br In vivo visualization of aromatase

  2024-12-24

  

  In vivo visualization of aromatase with positron emission tomography (PET) Positron emission tomography (PET) utilizes the high Modified GTP for DNA synthesis photons formed during the annihilation of positrons to detect the changes in the amount and localization of injected radiopharmaceuticals

• Arginase deficiency is a rare urea cycle disorder with

  2024-12-24

  

  Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a

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