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There is no doubt that
2021-10-23

There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago
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Compound was synthesized in a racemic fashion with this stud
2021-10-23

Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position
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GPR co localizes with ghrelin in the duodenum
2021-10-23

GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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Acknowledgments We would like to thank Dr Greg
2021-10-23

Acknowledgments We would like to thank Dr. Greg Morriello, Mr. Lehua Chang, Mr. Chris Moyes and Mr. Nam Fung Kar for intermediate 3 syntheses. Cheng Zhu would like to thank Dr. Milana Maletic, Mr. Kake Zhao and Mrs. Wanying Sun for helpful discussions. Introduction Glucagon-like peptide-1 (GLP-
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AKT inhibitor VIII We tested this hypothesis with two exper
2021-10-23

We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 AKT inhibitor VIII (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected systemically
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In summary we have developed an efficient synthetic route to
2021-10-23

In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ-
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Petrat et al could show that even a low
2021-10-23

Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c
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Taking into account abovementioned vitamin
2021-10-23

Taking into account abovementioned, vitamin D3 deficiency effects on synaptic neurotransmission can be considered as targeting both Ca2+-independent and Ca2+-dependent processes. Ca2+-independent action of vitamin D3 deficiency is associated with a decrease in the expression of glutamate and GABA tr
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Methods br Results br Discussion In this report the therapeu
2021-10-23

Methods Results Discussion In this report, the therapeutic effect of a GCGR antagonistic antibody REMD2.59 was tested in 2 mechanistically divergent disease models of heart failure without confounding defects in global metabolism. Based on histological and functional analyses in both MI-injur
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Prion diseases are transmissible and result in fatal
2021-10-23

Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in KU-57788 lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, can form fi
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Interestingly the subcellular localization of
2021-10-22

Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule 52 6 reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the ability of
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The present study was therefore conducted with three aims
2021-10-22

The present study was therefore conducted with three aims; (1) we tested the effect of IRL-1620, a selective ETB receptor agonist, on the analgesic tolerance to morphine and oxycodone in mice; (2) we determined the expression of ETA receptors and ETB receptors in the Zanamivir of morphine and oxyco
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br Histamine and glycaemia Histamine is involved in
2021-10-22

Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of CEP-37440 and diabetes date back to the 1950s. Since that time the involvement of histamine in diabe
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Interestingly myorelaxation and the stimulation of cGMP prod
2021-10-22

Interestingly, myorelaxation and the stimulation of cGMP production are properties also reported for sGC stimulators, such as YC-1 and BAY 41–2272 (i.e., indazole compounds that were discovered in the 1990s) [35]. They relax aortic ring contractions induced by phenylephrine, and their effects are si
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There are five subfamilies of P type ATPases I
2021-10-22

There are five subfamilies of P-type ATPases (I-V), which transport metal ions or phospholipids across membranes (Palmgren and Nissen, 2011). Although our studies indicate that the P-type ATPase domain is important for function, how it contributes to cGMP production is currently unknown. The P-type
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