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Selective pharmacological inhibition of tonic currents indic
2022-03-29

Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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Results from the current study are not consistent with those
2022-03-29

Results from the current study are not consistent with those of a previous study (Poock et al., 2015) where there was no differences in ovulation induction response when there was administration of gonadorelin hydrochloride and gonadorelin diacetate salts. These differences in results are likely due
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Mongolian gerbils Meriones unguiculatus a social rodent spec
2022-03-29

Mongolian gerbils (Meriones unguiculatus), a social rodent species, are widely distributed in the typical steppe, desert steppe and desert habitats of northern China, Mongolia, and Trans-Baikal region of Russia. In wild, the recorded maximum lifespan (apparent longevity) was 29.5 months for female M
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Introduction Substantial body of evidence supports the notio
2022-03-29

Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that
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br Acknowledgments This work was supported
2022-03-29

Acknowledgments This work was supported by the Slovak grant agency VEGA, Grant 2/0084/13. We would like to thank Dr. J. Bauer for careful reading of the manuscript. Introduction Glycine is an important neurotransmitter which regulates both Erastin inhibitory neurotransmission and excitatory
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Several studies have shown that regulation of
2022-03-29

Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upregu
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In order to test whether the enhanced
2022-03-29

In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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The atomic model of Ce INX
2022-03-29

The atomic model of Ce-INX6 provides an additional interpretation to the Ce-INX6ΔN mutant structure at low-resolution [41]. Given that the N-terminal residues from 2 to 19 are deleted in the Ce-INX6ΔN mutant, the N-terminal funnel found in the pore of the wild-type Ce-INX6 should be lost in the Ce-I
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Some but not all GSIs inhibit signal peptide peptidases as
2022-03-29

Some, but not all, GSIs inhibit signal peptide peptidases as well, though this has not been systemically studied [36], [41]. When considering biological activities of various GSIs this is an important and understudied caveat that could influence both biological response as well as potential toxiciti
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At the end of experiments
2022-03-29

At the end of experiments rats were injected high dose of sodium pentobarbital (90mg/kg) and the rat’s head was cut and frozen in −20°C for 20min with the injecting tube in situ before section. The location of the tip of the injecting tube was verified and all the tips of the injecting tube were in
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Similarly spectrophotometric titrations were carried out und
2022-03-29

Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant GDC-0084 band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a bathochromic shift of th
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In summary the SAR of a
2022-03-29

In summary, the SAR of a series of phenylpropanoic acid-free fatty ana 2 receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust efficacy in
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In cardiomyocytes mechanical stress builds up
2022-03-28

In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a trans
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Finally the optimized leads and were tested in rat
2022-03-28

Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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br Although earlier studies had reported conflicting results
2022-03-28

Although earlier studies had reported conflicting results regarding the role of Ca2+ in regulating SV endocytosis, more recent data suggest that Ca2+ influx facilitates SV endocytosis in hippocampal neurons, the calyx of Held, and in inner hair SC-10 (Dittman and Ryan, 2009, Hosoi et al., 2009, M
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