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The Rho family of GTPases is composed
2022-06-07
The Rho family of GTPases is composed of many small ubiquitous signaling G proteins that bind to guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). They act as switches: when binding to GTP, they are active and associate with a variety of target proteins that regulate intr
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Considering their good FAAH inhibitory activity compounds an
2022-06-07
Considering their good FAAH inhibitory activity, compounds and have been selected for an in vivo study in a DSS-induced colitis model. Specific Pathogen Free male 7weeks old C57/Bl6 mice received 2.5% DSS in drinking water during 8days. Concomitantly, they were administrated daily intraperitoneall
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Glycine released from astrocytes as well as neurons is
2022-06-07
Glycine released from astrocytes as well as neurons is also known as a co-agonist of NMDAR (Roux and Supplisson, 2000). Neuronal glycine in mouse hippocampus might be released from glutamatergic terminals (Muller et al., 2013) that express functional GSK2334470 receptors (Rodriguez et al., 1997). G
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Introduction Histamine Imidazolyl ethylamine is an
2022-06-07
Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric Dequalinium Chloride secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histam
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Bile acids synthesized in the liver are
2022-06-07
Bile acids synthesized in the liver are secreted into the intestinal tract to facilitate the digestion and Vicriviroc Malate of nutrients. Most bile acids are reabsorbed by the ileum and are transported back to the liver via the portal blood circulation. Recently, bile acids have also been consider
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Three additional Type I CDK and CDK kinase inhibitors
2022-06-07
Three additional Type I CDK8 and CDK19 kinase inhibitors have also been recently reported. Orally available 3-benzylindazole 12 was discovered by optimization of compounds with HSP90 affinity to yield potent and selective CDK8 inhibitors. Compound 12 showed strong binding activity for CDK8 with an I
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br Conclusion Interactions between neurons and astrocytes de
2022-06-07
Conclusion Interactions between neurons and astrocytes depend on the spatial configuration of their contacts. Therefore, changes of astrocyte morphology may impact various physiological mechanisms ranging from glutamate uptake and potassium homeostasis to modulation of synaptic transmission and p
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In summary we have successfully identified
2022-06-07
In summary, we have successfully identified a series of potent and selective GSNOR inhibitors having imidazole and tetrazole functional groups in both end of the core structure and many compounds have been identified with IC: Introduction Peppers (Capsicum annuum L.), tomatoes and potatoes, belon
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br Acknowledgments We thank Dr
2022-06-07
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 Deoxycholic acid expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. An
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We recently reported the first cyclopropene analog of
2022-06-06
We recently reported the first cyclopropene-analog of the amino Conclusions neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [28]. W
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The unique mechanism of EAAT anion
2022-06-06
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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GHRL effect on appetite is influenced by its dose and
2022-06-06
GHRL effect on appetite is influenced by its dose and route of administration, where central or peripheral administration of GHRL at low doses increases feed intake, via acting on orexigenic hypothalamic neurons, and decreases appetite at high doses in chickens (Jonaidi et al., 2012), quails (Shoush
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Comparison of dlGALRs deduced amino acid
2022-06-06
Comparison of dlGALRs deduced amino ABT-869 sequences with that of human GALRs demonstrate that the GALR1 ortholog sequences have diverged less than those of GALR2. Since often duplicate genes undergo divergent evolution through sub-functionalization, loss or gain of new functions (Prince and Picket
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We hypothesize that HBO increases GABA
2022-06-06
We hypothesize that HBO2 increases GABA activity at the GABAA receptor via a nitric oxide dependent mechanism. Blotting for the phosphorylated β3 subunit of the GABAA receptor should theoretically be increased when there is more GABA activity at the receptor (McDonald et al., 1998). We expected that
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The present data suggest that the
2022-06-06
The present data suggest that the decrease of liver BAs was mainly due to the decrease of hepatic BAs synthesis because the BA synthetic enzymes Cyp7a1, Cyp7b1 and Cyp8b1 were markedly reduced. The increase may also be due to the increase of hepatic BAs efflux, because the liver BA efflux transporte
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