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The overall very satisfactory potency profile of compounds a
2021-12-21
The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic SBI-0206965 core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly s
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Brain derived neurotrophic factor BDNF is
2021-12-21
Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of
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br Introduction Stroke is the second cause of death
2021-12-20
Introduction Stroke is the second cause of death worldwide and the first cause of acquired motor disability in adults [1], [2]. In sub-Saharan Africa, stroke is the first cause of admission in neurology departments [3]. In Cameroon, the in-hospital mortality of stroke is estimated at 26.8% [4]. A
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Our results demonstrated that most of the HUA
2021-12-20
Our results demonstrated that most of the HUA rings incubated with 100 μM TBT do not have the capacity to contract in the presence of 5-HT or exhibit very low contractions in comparison to the control. Only 23.3% of the HUA rings were able to contract. These results seem to indicate that there may b
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Platycodon grandiflorum is a member of the genus
2021-12-20
Platycodon grandiflorum is a member of the genus Platycodon and is commonly known as balloon flower. In East Asia, P. grandiflorum is used for the treatment of asthma, coughs, inflammatory diseases, pulmonary tuberculosis, and diabetes (Takagi and Lee, 1972). Furthermore, recent studies have reporte
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br For some time it
2021-12-20
For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor 1664 in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on the regulation
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br Conclusion br Author contributions br Competing interests
2021-12-20
Conclusion Author contributions Competing interests Acknowledgments Introduction Reproductive performance is a major factor affecting profitability of dairy farms. The use of GnRH and prostaglandin F2α (PGF2α) in a coordinated fashion allows cows to be inseminated as a result of the u
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br Endogenous lipids as SLC transporter modulators Lipids
2021-12-20
Endogenous lipids as SLC6 transporter modulators Lipids constitute part of the environment in which membrane-embedded transporters operate [62]. Endogenous lipids can act as inhibitory ligands [63] or functionally important components of the membrane that impart changes in transporter structure [
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The functionally crucial arginine within M is not encoded
2021-12-20
The functionally crucial arginine within M2 is not encoded by the gluR2 gene, but rather arises within the pre-mRNA by editing of a codon for the neutral glutamine residue25, 26. RNA editing at the Q/R site is specific to GluR2 and is extremely efficient. In neonatal and adult rat brain, almost 100%
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Moreover after the initial bleaching of the
2021-12-20
Moreover, after the initial bleaching of the fluorescent molecules in the targeted cell exposed to laser illumination, the neighboring reservoir pyk2 are expected to give in return new fluorescent ones if the cells are coupled together by gap junction channels. This supposes that the level of fluore
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One major issue has dominated studies
2021-12-20
One major issue has dominated studies of the nematode connectome: its reproducibility. The difficulties that had to be surmounted just to assemble a complete wiring diagram precluded comparisons of the complete wiring from several different animals. Instead the earliest adult hermaphrodite wiring di
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br Conflict of interest br Acknowledgment M D
2021-12-20
Conflict of interest Acknowledgment M.D.P. lab is supported by the EPFL and Swiss National Science Foundation (SNF grant No. 200020_157153). Introduction As amyloid-β peptide (Aβ) accumulation in the melatonin receptor agonists starts in the very early stages of Alzheimer’s disease (AD) p
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br ACKNOWLEDGMENTS br Introduction Odorant
2021-12-20
ACKNOWLEDGMENTS Introduction Odorant receptors (ORs) are the largest subfamily of G protein-coupled receptors (GPCRs) and are mainly expressed by olfactory sensory neurons in the nose for the detection of various odorants [1]. However, more recent reports suggest that ORs are also expressed an
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br G protein coupled receptor GPR also known
2021-12-20
G-protein coupled receptor 40 (GPR40), also known as a free fatty parp apoptosis pathway receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that GPR
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br Results br Discussion In this
2021-12-20
Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of BMS265246 unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in the fina
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