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In conclusion we have shown that
2021-10-13

In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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toremifene br Acknowledgments We thank Drs Yasuhiro Saito an
2021-10-13

Acknowledgments We thank Drs. Yasuhiro Saito and Mitsuru Futakuchi for helpful discussion. We also thank Drs. Kohei Miyazono and Tadashi Matsuda for cells. This work was supported by Grant-in-Aids for Scientific Research on Innovative Area (16H06373; 16K15273) from MEXT, Japan (to M.H.) and by Pr
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Apigenin trihydroxyflavone a natural plant flavone is a bioa
2021-10-13

Apigenin (4′, 5, 7-trihydroxyflavone), a natural plant flavone, is a bioactive compound present in a variety of fruits, vegetables, and medicinal plants, and its various beneficial biological activities have been reviewed (Zhou et al., 2017), including HIF-1α inhibition-mediated anti-tumor. Recently
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Of what interest is the
2021-10-13

Of what interest is the link between GSNOR and NO in the plant response to Fe deficiency? On the one hand, NO acts as an important signal to help plants accommodate Fe deficiencies; on the other hand, surplus NO is indeed a harmful RNS that induces severe S-nitrosylation-related damage at a higher s
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Several studies have found that GPR possesses a
2021-10-13

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected BIX 01294 mg expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A
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Because of the commercial availability of some acetamide
2021-10-13

Because of the commercial availability of some acetamide phenol starting materials, a few acetamide final products (such as and , ) were directly synthesized via a Mitsunobu reaction with chloropyrimidine piperidinyl cyclopropyl alcohol . The 3-pyridinyl analogue was synthesized by a nucleophilic ar
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While NR upregulation in the spinal cord is
2021-10-13

While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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br Materials and methods br
2021-10-13

Materials and methods Results Discussion Neurotransmitter uptake is one of the most important aspects of synaptic transmission, it fact, the existence of a specific uptake system is one of the requisites that any neuroactive substance has to cover to be considered a neurotransmitter. It has
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br Material and methods br Results br Discussion Accumulatin
2021-10-13

Material and methods Results Discussion Accumulating evidence suggests that the hippocampus is sensitive to noise-induced hearing loss and other forms of sensory deprivation, which deprives the hippocampus of sensory information required for its normal operations such as spatial navigation
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In cardiomyocytes mechanical stress builds up via FAs and
2021-10-12

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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In addition to Rabs several
2021-10-12

In addition to Rabs, several proteins have been shown to interact with Rabphilin3a, for instance the GluN2A subunit of the NMDA receptor, PSD-95 ([56,57] and references therein), Rabaptin-5, α-actinin [16] and SNAP-25 [21,23,41,61]. Only the latter has been reported to participate in the AR. Explori
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br Although earlier studies had reported conflicting results
2021-10-12

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 O6-Benzylguanine receptor (Dittman and Ryan, 2009, H
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Several named antagonist ligands have figured noticeably in
2021-10-12

Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l
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Biochemical and genetic studies indicate that the
2021-10-12

Biochemical and genetic studies indicate that the endosomal sorting complex required for transport (ESCRT) machinery is crucial for Hh exovesicle packaging and morphogen gradient function 39., 43., 44.. In vertebrates, ESCRT proteins promote the release of Shh exovesicles to maintain progenitor cell
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br Materials and methods br
2021-10-12

Materials and methods Results Discussion D. abbreviatus larvae are voracious feeders, and the nutrients consumed as part of their diet are broken by gut proteases and utilized for growth and development. Since proteases play an important role in larval and adult food digestion, it is import
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