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br Acknowledgments We would like
2021-12-18

Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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Inhibitors of the G rdos effect include the Ca channel
2021-12-18

Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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In the last thirty years accumulating
2021-12-17

In the last thirty years, accumulating data have addressed a role for GABA in the modulation of gastrointestinal (GI) functions via its possible involvement in the circuitry of the enteric nervous system (ENS). The ENS is a complex neuronal network located within the gut wall, capable of regulating,
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The RAS RAF MEK ERK pathway also known as
2021-12-17

The RAS/RAF/MEK/ERK pathway (also known as the MAPK/ERK pathway) is one of the most important signaling pathways in PDAC. Activation of the MAPK/ERK pathway promotes PDAC growth and apoptosis resistance in response to gemcitabine [43,44]. We previously demonstrated that inhibition of GPX4 can overco
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Data of initial analogs have been shown in
2021-12-17

Data of initial analogs (±)-– have been shown in wherein SAR was observed for the intended change of the right-hand side pyridin-3-yl ring of to various other -containing heteroaryl ring (Ar) disposing the ring- at different directions. Based on consistent human and rat FAAH potency as well as intri
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The present study was designed to clarify the distribution a
2021-12-17

The present study was designed to clarify the distribution and the function of the endothelin receptors in the guinea-pig urinary bladder. We found that endothelin-1 produced a clear tonic contraction via both PD 151746 mg subtypes, the endothelin ETA and ETB receptor, and that sarafotoxin S6c also
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Compared to the other histamine
2021-12-17

Compared to the other 3-Deazaadenosine receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (200
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br Introduction The signaling molecule nitric
2021-12-17

Introduction The signaling molecule nitric oxide (NO) plays an essential role in vessel homeostasis by initiating vasodilation [1], [2], [3]. After biosynthesis in endothelial cells, NO diffuses into the subjacent smooth muscle layer to reach its target enzyme, soluble guanylyl cyclase (sGC, EC 4
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Many studies have reported on the association between
2021-12-17

Many studies have reported on the association between GST gene polymorphisms and pulmonary disorders but with controversial results [7]. In the present study, on comparing results of GSTP1 gene polymorphism among the studied COPD patient groups, it was found that heterozygote mutation was significa
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The GPR receptor is also emerging as an important therapeuti
2021-12-17

The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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br Material and methods br Results Consistent with our
2021-12-17

Material and methods Results Consistent with our previous study, SR-SIM and confocal microscopy showed a large number of IBA1-expressing TKI-258 in all parts of the human cochleae (Fig. 1). IBA1, the microglial and macrophage-specific calcium-binding protein, is involved in the membrane ruffli
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Dendritic damage and loss of synaptic connections correlate
2021-12-17

Dendritic damage and loss of synaptic connections correlate with cognitive decline in HAND patients. Synapse loss induced by HIV proteins occurs early and via a different signaling pathway from that leading to neuronal death (Kim et al., 2008), suggesting that synapse loss might be a mechanism to re
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In parallel we were also
2021-12-17

In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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br Introduction Herpes viruses are members of
2021-12-17

Introduction Herpes viruses are members of Herpesviridae family. This family consists of DNA viruses and it is a very large family. The viruses related to this family cause many diseases in animals and humans [1]. Herpes simplex viruses cause mucocutaneous lesions in the affected humans. These l
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Because of the relationship between carbohydrate consumption
2021-12-17

Because of the relationship between carbohydrate consumption and chronic diseases such as obesity and type II diabetes (Hu, van Dam, & Liu, 2001), there is mounting interest to evaluate the quality of GSK J4 receptor through analysis by glycemic index (GI) and Englyst assay, for example (Englyst, K
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