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The comparatively low number of H R
2021-12-13
The comparatively low number of H1R agonists is contrasted by the high number of diverse H1R antagonists. Based on pharmacological classification, they are grouped into different generations by considering their target as well as side effects profile. The first generation “antihistamines” consist of
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It appears that not all GPR agonists require a
2021-12-13
It appears that not all GPR119 agonists require a high dose to elicit acceptable Pregnenolone Carbonitrile receptor control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those
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Introduction GPR is a class A type
2021-12-13
Introduction GPR119 is a class A type of G Protein coupled receptor, which is expressed primarily in pancreatic β-cells and the K and L Olomoucine australia of the gastrointestinal tract [1], [2], [3]. Activation of GPR119 promotes secretion of incretins such as glucagon-like peptide-1 (GLP-1) in
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It is well known that the
2021-12-13
It is well known that the expression of GPR109A is regulated under physiological and pathological conditions. We previously found that GPR109A expression in islet beta-cells increased with age and was up-regulated by interferon-γ (Li et al., 2011). GPR109A levels in Min6 and INS-1E islet beta-cells
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Overall ABC transporters are hypothesised to prevent the
2021-12-13
Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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The glucocorticoid GR complex exerts wide spread
2021-12-13
The glucocorticoid-GR complex exerts wide-spread cellular effects through two distinct mechanisms categorized as genomic and non-genomic pathways [3,39]. Most non-genomic pathways originate from activation of mGR [40]. These actions of the GR appear to all play an important role in the regulation of
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Genetic disruption or pharmacologic inhibition of
2021-12-13
Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co
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Introduction br Alzheimer pathology A and Tau Amyloid
2021-12-13
Introduction Alzheimer pathology: Aβ and Tau Amyloid β protein (Aβ) plays an important role in AD pathogenesis. At the molecular level, senile amyloid plaques and neurofibrillary tangles (NFT) are two neuropathological hallmarks of AD [1]. Mutations in genes encoding amyloid precursor protein (A
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Most of the above mechanisms are implicated in
2021-12-13
Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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In terms of cytotoxicity studies under two dimensional
2021-12-13
In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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NeuroHIV is initiated by HIV crossing the blood brain barrie
2021-12-13
NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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br Methods br Acknowledgements We are grateful to
2021-12-10
Methods Acknowledgements We are grateful to Eric Olson for providing Yap/Taz floxed mice, and to members of the Epstein lab for helpful comments and advice. This work was supported by NIH R01 HL118768, R35 HL140018, the Cotswold Foundation and the WW Smith Endowed Chair to J.A.E. The Hippo
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Interestingly in vivo infusion and uptake of Ang II in
2021-12-10
Interestingly, in vivo infusion and uptake of Ang II in intact mice indicated that multiligand endocytic receptor megalin has at least some role in the uptake of Ang II and the downstream signaling process in proximal tubule Carprofen (PTCs) in vivo [173]. Earlier in vivo studies showed that PTCs o
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To apply the recently developed
2021-12-10
To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the VU 591 hydrochloride and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To thi
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DNAzymes a series of nucleotide sequences
2021-12-10
DNAzymes, a series of nucleotide sequences with specific catalytic activity, have been reported frequently applied in detection assays for such as ions and amino acids, due to the advantage in stability, high cost-effectiveness and modification convenience, by comparison with protein enzymes. The DN
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