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H R antagonism can prevent
2021-09-29
H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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Tourette s syndrome TS is a neurobehavioral disorder charact
2021-09-29
Tourette's syndrome (TS) is a neurobehavioral disorder characterized by chronic motor and vocal tics. The histaminergic system appears to be implicated in the pathophysiology of TS because H3R up-regulation has been observed in the striatum of HDC knock-out animal models (Rapanelli et al., 2017; Rap
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Posttraining memory facilitation by histamine infused into t
2021-09-29
Posttraining memory facilitation by histamine infused into the dorsal hippocampus was also observed in two more recently described and very important non-aversive forms of memory: object recognition (da Silveira, Furini, Benetti, Monteiro, & Izquierdo, 2013) and social recognition (Garrido Zinn et a
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br HER proto oncogene The erbB
2021-09-29
HER2 proto-oncogene The erbB2 gene, located on the short arm of chromosome 17, was discovered and cloned in 1983 (Fig. 1) (Sato et al., 1983). The product of this gene, HER2, is a transmembrane glycoprotein of 185 KDa that consists of three main domains: an extracellular, a transmembrane and an i
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In summary we have designed and optimized
2021-09-29
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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For molecules with potential for
2021-09-29
For molecules with potential for therapeutic use, high potency is desired, preferably in the nM or lower concentration range. However, the glycine receptor specific peptides identified with the New England Biolabs Ph.D. libraries, both in this study (Fig. 3) and by Tipps et al. (2010), acted at low
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br Regulation of Glu transporters
2021-09-29
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Bexarotene calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcrip
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Previous reports have showed that
2021-09-29
Previous reports have showed that the expression and localization of GLUT8 in mouse (Gómez et al., 2006; Kim and Moley, 2007), rat (Ibberson et al., 2002) and human (Schürmann et al., 2002). In this study, GLUT8 protein mainly localized in the spermatocytes, elongated and round spermatids in the adu
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Cytokines and hormones influence both gap junctions and endo
2021-09-28
Cytokines and hormones influence both gap junctions [106] and endocrine activity in the pituitary [3]. Long-term treatment (2 h) with the proinflammatory cytokines interleukin-1β (Il-1β) and tumor necrosis factor-α (TNF-α) transiently increases Cx43 expression and cell coupling in TtT/GF Gadodiamide
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Brain derived neurotrophic factor BDNF is the
2021-09-28
Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of
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Whether histamine receptor distribution is altered in canine
2021-09-28
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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a cool way to improve Introduction As a compound class histo
2021-09-28
Introduction As a compound class, histone deacetylase inhibitors (HDIs) have been remarkably successful in the treatment of T-cell lymphoma [1]. Vorinostat (suberanilohydroxamic a cool way to improve or SAHA) was approved by the FDA in 2006 for the treatment of cutaneous T-cell lymphoma [2], [3];
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br Experimental br Acknowledgment br Introduction Hepatitis
2021-09-28
Experimental Acknowledgment Introduction Hepatitis C virus (HCV) belongs to Flaviviridae, is a blood-borne pathogen which infects about 180 million individuals throughout the world; most of the cases lead to end stage liver diseases, fibrosis, cirrhosis and hepatocellular carcinoma (Choo et
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In order to study the role of
2021-09-28
In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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GPR belongs to the G protein coupled receptor
2021-09-28
GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty bms-690514 (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expressed in bone marrow
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