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We observed the reduced expression of the
2022-03-21

We observed the reduced expression of the GluN2a subunit in the temporal and entorhinal cortexes and ventral hippocampus, which may result in the predominance of GluN2b-containing NMDA receptors during the latent period. Previously, using the same model, we revealed the reduction of the GluN2a/GluN2
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br The hippocampus and spatial memory
2022-03-21

The hippocampus and spatial memory Numerous lines of evidence have implicated the rodent hippocampus in spatial forms of learning and memory (O’Keefe and Nadel, 1978). For example, hippocampal lesions produce robust and reliable deficits on spatial memory tasks such as the Morris watermaze in bot
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Next the effects of a phenyl group at the
2022-03-21

Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio
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br In vivo actions of GLP
2022-03-21

In vivo actions of GLP-1/GLP-1R agonists on the vascular endothelium Using contrast-enhanced ultrasound, male Sprague Dawley rats receiving an intravenous infusion of native GLP-1 (30 pmol/kg/min) for 2 h demonstrated significant improvements in both microvascular blood volume and microvascular b
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br Hedgehog HH signaling plays an important
2022-03-21

Hedgehog (HH) signaling plays an important role both during embryonic development and adult life. It is involved in the regulation of cell differentiation, cell proliferation and tissue polarity, as well as in the maintenance of stem cells, tissue repair, and regeneration (, ). Three ligands, Indi
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In mammals the primary cilium is
2022-03-21

In mammals, the primary cilium is considered a hub for signal transduction. The cilium has previous been associated with transduction of several pathways including Wnt (Corbit et al., 2008, McDermott et al., 2010, Tran et al., 2014), PDGF (Clement et al., 2013, Schneider et al., 2010, Schneider et a
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br Introduction Connexins are transmembrane proteins that
2022-03-21

Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent artesunate mg via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nutrients to the extracel
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AGN 194310 These reports have gradually established G quadru
2022-03-21

These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio
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Another small compound targeting IBAT has
2022-03-21

Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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A general synthesis of the tetrazole is shown in
2022-03-18

A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic SCH772984 TFA synthesis followed by reduc
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Histone modification is one of the major epigenetic
2022-03-18

Histone modification is one of the major epigenetic mechanisms.8, 10 Specific histone modifications confer active or repressive transcriptional states. For instance, the trimethylation of Histone3-Lysine27 (H3K27me3) is a marker of tightly packaged heterochromatin and is associated with gene repress
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br Introduction Currently HIV infection treatment
2022-03-18

Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms
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Betahistine N methyl pyridyl ethylamine is a well
2022-03-18

Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 UCB 35625 agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for this
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br Trifluoromethylketones This group of compounds
2022-03-18

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc WAY 208466 dihydrochloride sale in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophen
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In the course of studies leading to
2022-03-18

In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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