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In experiments using D to displace binding of
2021-09-09
In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse Tanshinone I tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1, Fig. 2
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The developed method was used to quantify
2021-09-09
The developed method was used to quantify RBC membrane transport of the anomers of three monofluorinated analogs of glucose in a modified medium designed to provide stable metabolic properties of the cells over the lifetime of the experiment. This allowed us to evaluate the specific interaction (spe
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The general aim of our
2021-09-09
The general aim of our in vitro experiments was to analyze the patterns of ghrelin and GHSR-1a expression in the mammary glands of dairy goats during pregnancy and to examine the direct effect of ghrelin on cell proliferation in cultured MECs of pregnant dairy goats. For this purpose, we cultured go
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Newt GHS R a proteins expressed in a mammalian
2021-09-09
Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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Iodination of commercially available with excess ICl
2021-09-09
Iodination of commercially available with excess ICl in AcOH gave a quantitative yield of , which was cyclized with benzyl thioamides to give the 2-benzyl-9,10-dihydro-4-1-thia-3,4-diaza-benzo[]azulenes . Coupling of the iodides with heterocycles including imidazoles, triazoles, or zinc cyanide us
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The synthesis of compounds and were
2021-09-09
The synthesis of compounds and were achieved according to standard procedures. As shown in , The compound 4-methyl-1-(4-sulfobutyl)quinolonium () was prepared by alkylation reaction. Compounds and were synthesized by substitution reactions between 4-fluorobenzaldehyde and , , '-trimethylethanedi
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Contrary to the transient nature of signal transmission thro
2021-09-09
Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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We thus asked whether enhanced AEA levels in the
2021-09-09
We thus asked whether enhanced AEA levels in the Linezolid receptor reduce the level of age-related inflammatory changes and slow down brain ageing. To answer this question we compared the morphology of microglia and level of pro-inflammatory cytokines in the hippocampus of young and old wild-type
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The H R antagonist cimetidine Tagamet became the
2021-09-09
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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Fig illustrates the different signaling pathways
2021-09-09
Fig. 1 illustrates the different signaling pathways elicited or modulated by H3R activation. Collectively, the modulation of the release of histamine and other neurotransmitters through H3R activation could be linked to several neurological disorders such as sleep disorders like narcolepsy, Alzheime
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The translation of the HCV genomic RNA is initiated in
2021-09-09
The translation of the HCV genomic RNA is initiated in a different manner, referred to as internal initiation: the 40S subunit directly forms a binary complex with the HCV genomic RNA via an internal RNA sequence called IRES, which is located in the 5′-UTR (Pestova et al., 1998, Tsukiyama-Kohara et
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A motivation for this study is the
2021-09-08
A motivation for this study is the ability of PGD2 to inhibit hair lengthening (). Here we demonstrate that PGD2 also inhibits hair regeneration after wounding. Thus, PGD2 and Gpr44 inhibition of the hair follicle occurs in multiple contexts and may be exploited in future therapies. Pharmaceutical c
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Human GPR hGPR was originally
2021-09-08
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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For molecules with potential for therapeutic use
2021-09-08
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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The typical pharmacophore for GPR agonists contains
2021-09-08
The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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