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br Acknowledgments R Dalmann has obtained a bourse
2021-12-06
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
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Enhancer of zeste homolog EZH
2021-12-06
Enhancer of zeste homolog 2 (EZH2), which functions as a methyltransferase, is a critical subunit of polycomb repressive complex 2 (PRC2), which has been demonstrated to be involved in the development of the mct inhibitor [23]. Aberrant expression of EZH2 has been found to be associated with a vari
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Mammalian CAPS includes two i http www apexbt com
2021-12-06
Mammalian CAPS includes two isoforms, CAPS-1 and CAPS-2. Both isoforms contain several functional domains, including a C2 domain that is likely responsible for CAPS dimerization (Petrie et al., 2016), a pleckstrin homology (PH) domain that binds PIP2 (phosphatidylinositol 4,5-bisphosphate) and media
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AD is a major neurological disorder
2021-12-06
AD is a major neurological disorder, usually effecting the elderly population, which is difficult to diagnose until symptoms begin to accumulate. As of 2013, approximately five million Americans were living with AD. The number with this disease is projected to be 16 million by 2050 (Hebert et al., 2
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Gefitinib hydrochloride br Discussion This study dedicated t
2021-12-06
Discussion This study, dedicated to Gefitinib hydrochloride H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibitio
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Multi targeting agents are of major interest in
2021-12-06
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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To combat the detrimental effects of neuropathological condi
2021-12-06
To combat the detrimental effects of neuropathological conditions, additional therapeutic interventions that either dampen chronic neuroinflammation or attenuate reductions in hippocampal neurogenesis are critically needed. The cannabinoid system has already been shown to rescue impaired neurogenesi
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cytochalasin d After the synthesis of methylsulfonyl or tetr
2021-12-06
After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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Our inhibitor studies revealed the presence of a signaling
2021-12-06
Our inhibitor studies revealed the presence of a signaling network triggered by dicarbonyl stress. Nevertheless, p38-MAPK activation was clearly necessary for NADPH-oxidase mediated production of ROS. This is consistent with data from other groups using different cell culture systems [37], [38], [39
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Anderson et al reported a markedly decreased
2021-12-06
Anderson et al reported 5402 markedly decreased maladaptive behavior traits of the VABS maladaptive behavior score after using EAA (Equine Assisted Activities) (F(1,11) = 5.65, = 5.65, (F(1,11) = 5.19, p = 0.04). However, the results of other EQ/SQ parts and of the VABS correlated with EAA did not
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To confirm that these were bona fide
2021-12-06
To confirm that these were bona fide interactions, we investigated whether the potassium channel subunits or Tmem263 formed complexes with GLT-1 or DAT after immunoprecipitation. Lysates of HEK-293 cells previously cotransfected with HA-GLT-1 or HA-DAT, and either YFP-Kv7.3, YFP-Kv7.2 or YFP-Kv7.5 w
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A number of anti diabetic drugs
2021-12-06
A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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Exposure of human and animals to MPTP can reproduce
2021-12-06
Exposure of human and animals to MPTP can reproduce all the characteristic motor and non-motor signs of PD, in addition to mimicking the same responses and side effects to drugs used to treat PD [37], [38]. Anatomically, intoxication with MPTP induces the same selective loss of substantia nigra DA n
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So far several methods have been
2021-12-06
So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute daunorubicin mg slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels or on “dye coupling” experim
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Since our new compound Fex could
2021-12-04
Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 primaquine phosphate with transwell experiments. Fro
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