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Human GPR hGPR was originally isolated in as an orphan
2022-10-04
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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Excessive adiposity is also a key pathogenic
2022-10-04
Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP
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The unique mechanism of EAAT anion channel gating results
2022-10-04
The unique mechanism of EAAT anion channel gating results in neuronal or glial anion conductances that follow changes in substrate concentrations and thus allow feedback control of glutamate release (Wersinger et al., 2006) or modification of GABAergic postsynaptic currents by glutamatergic signals
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GLI proteins activate or repress transcription of their targ
2022-10-03
GLI proteins activate or repress transcription of their target genes by binding to a similar sequence motif within a cis-regulatory module (CRM) (Hallikas and Taipale, 2006, Peterson et al., 2012). Transcriptional responses to the HH pathway can be elicited either by de-repression of GLI-R or in oth
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Dysregulation of the HPA axis
2022-10-02
Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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The first suggestion that histamine may play a role in
2022-10-02
The first suggestion that histamine may play a role in memory consolidation was from Almeida and Izquierdo (de Almeida & Izquierdo, 1986) who showed that the immediate posttraining intracerebroventricular (i.c.v.) administration of 1–10ng of the drug were found to enhance the retention of one-trial
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In first wave first generation drugs telaprevir and boceprev
2022-10-01
In 2013, first-wave, first-generation drugs telaprevir and boceprevir was the first protease inhibitors (PIs) incorporated in Brazilian Clinical Guidelines for the treatment of patients infected with HCV Bacitracin 1. Based on this 2013 Clinical Guideline, telaprevir could be used for both naïve an
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Among the GSK inhibitors available in market lithium
2022-10-01
Among the GSK-3 inhibitors available in market, lithium is probably the only example and the oldest one. Some molecules, both natural and synthetic, such as maleimide derivatives, staurosporine (from the bacterium Streptomyces storosporeus), indole derivatives such as indirubin (used since long in t
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hGPR was mapped to human chromosome
2022-10-01
hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen, and striatum (Sawzdargo et al., 1999). In rats, in situ hybridization indicated expression in hippocampus, thalamus and regions of the midbrain (Sawzdargo et al., 1999). Ryberg et
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Interestingly mGlu and mGlu receptors
2022-09-30
Interestingly, mGlu2 and mGlu3 receptors differ notably by their cellular distribution. Whereas mGlu2 receptors are mostly neuronal, mGlu3 receptors are expressed both in glia and in neurons. In neurons, mGlu3 receptors are present at the post-synapse and in presynaptic elements (Tamaru et al., 2001
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br Characterization and regional localization of Glu transpo
2022-09-30
Characterization and regional localization of Glu transporters Molecular studies led to the description of five subtypes of plasma membrane Glu transporters termed in accordance to their human or rodent origin (Kanai and Hediger, 1992, Pines et al., 1992, Storck et al., 1992). In humans, these tr
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Here we reported series of carbohydrate
2022-09-30
Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of Calpeptin and their polyol structures give them many unique biological properties as we have described earlier. More int
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The primary requirements of an ideal bioprobe for
2022-09-30
The primary requirements of an ideal bioprobe for glucose transporter-mediated bioimaging include high specificity, sensitivity as well as low cytotoxicity [18]. According to these concepts, we recently reported the simple amide linked glycoconjugates which containing cyanine fluorophores (Cy3 and C
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br Conflict of interest br Acknowledgements br Introduction
2022-09-30
Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2
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Phylogenetic analysis of the secretin like hormones yields
2022-09-30
Phylogenetic analysis of the secretin-like hormones yields poorly supported trees due to the short length of their peptide sequences (Dores et al., 1996). However, phylogenetic analyses typically show that the secretin-like peptides encoded by the proglucagon (glucagon, GLP-1 and GLP-2) and GIP endo
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