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The histamine H receptor H R
2022-08-08
The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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It is important to mention that the IC
2022-08-08
It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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br Although there are growing
2022-08-08
Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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The different NO stimulated and ODQ inhibited cNMP
2022-08-05
The different NO-stimulated and ODQ-inhibited cNMP patterns in terms of absolute and relative magnitude and time course reported herein suggest distinct functional roles of cGMP, cCMP and cUMP. Therefore, it will be necessary to dissect cellular effects of these cNMPs in numerous cell systems. For t
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Hypoxia has been shown to affect miR
2022-08-05
Hypoxia has been shown to affect miR-155 expression that can induce autophagy in nasopharyngeal and cervical carcinoma cells [334]. Suppression of miR-155 inhibited hypoxia-induced autophagy. miR-155 targeted mRNAs involved in the PI3K/PTEN/Akt/mTORC1 pathway including: Ras homolog enriched in Ergos
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INTRODUCTION Scar formation and tissue
2022-08-05
INTRODUCTION Scar formation and tissue regeneration are opposite results of the wound healing process. Although fibrosis is more common after skin injury, full skin regeneration results in complete replacement of adnexa and function. Examples of tissue regeneration in mammalian systems include annu
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Before cell motility assay cells
2022-08-05
Before cell motility assay, Fosaprepitant dimeglumine salt sale were pretreated with GW1100 (1 μM), which is an antagonist of GPR40 [20], [21]. GW1100 increased the cell motile activity of MG63-R7 cells in the presence of GW9508, similar as observed with MG-63 cells (Fig. 4A). Moreover, to confirm t
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Rapid action of E on GnRH neurons has
2022-08-05
Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor
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It is important to clarify whether
2022-08-05
It is important to clarify whether the decrease in USV after administration was secondary to the central depressant actions of the test compounds. Several reports have addressed the possibility that central depressant actions such as motor incoordination or changes in body temperature might affect U
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Although the overall structures of mGlu and mGlu VFTs
2022-08-05
Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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With these cyclopropene glutamate derivatives in hand we
2022-08-05
With these cyclopropene-glutamate derivatives in hand, we tested their ability to ligate with popular bioorthogonal reagents (Fig 3). First, we tested their ability to ligate with a tetrazine (3,6-Di-2-pyridyl-1,2,4,5-tetrazine) via an inverse electron demand Diels-Alder reaction by monitoring the
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In agreement with the results obtained
2022-08-05
In agreement with the results obtained from GluR-A−/− mice, mice in which the NR1 subunit of the NMDA receptor has been selectively deleted from the CA3 subfield of the hippocampus displayed normal acquisition of the standard reference memory version of the watermaze task (Nakazawa et al., 2002), bu
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In the present study a significant increase in liver glut
2022-08-05
In the present study, a significant increase in liver glut4 mRNA levels as well as an increase in liver glycogen content was observed in the dogfish in response to glucose-loading, although we did not observe any changes in liver glycogen content or glut mRNA levels following insulin administration
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br Results and Discussion br STAR Methods
2022-08-05
Results and Discussion STAR★Methods Author Contributions Conflicts of Interest J.P.F. is a consultant for AstraZeneca, BMS, Johnson and Johnson, Novo Nordisk, and Sanofi, a member of the advisory panel for AstraZeneca and Sanofi, a member of the speaker’s bureau for Sanofi and Novo Nordi
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Thirteen multiparous German Holstein cows
2022-08-04
Thirteen multiparous German Holstein cows, in their second to fourth lactation, were selected from a previous study (Schäff et al., 2012) based on their individual peak in plasma BHB concentrations in wk 2 or 3 postpartum: high BHB (H-BHB; 1.05 to 2.57 mmol/L, mean 1.59 mmol/L; n = 8) and low BHB (L
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