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br Discussion This study dedicated to histamine H and H
2021-09-15
Discussion This study, dedicated to NG25 H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibition of transmitter rel
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Multi targeting agents are of major
2021-09-15
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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br Hippo pathway signalling The Hippo pathway is an
2021-09-15
Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular hippo signaling status [10]. This pathway is linked to development, cell prol
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Interestingly the virulence of HBV may
2021-09-15
Interestingly, the virulence of HBV may adaptively evolve, thus affecting the macroscopic propagation of hepatitis B. Higher virulence in vivo may result in a higher transmission rate and mortality. By assuming that the transmission rate is a monotonically increasing function of virulence, , we pro
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br Conclusions br Acknowledgments This work
2021-09-15
Conclusions Acknowledgments This work was financially supported partly by Shanghai Pujiang Talent Project (No.: 08PJ14017), the National Natural Science Foundation of China (Nos.: 20771029 and 91013001) and Shanghai Leading Academic Discipline Project (No. B108). Soluble guanylate cyclase (
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br Material and methods br Results and discussion Unlike
2021-09-15
Material and methods Results and discussion Unlike many fruits such as bananas and tomatoes, known as climacteric fruits, in which ripening is regulated by a burst of STF 083010 synthesis biosynthesis and an increase in respiration, pepper fruits, which do not follow this pattern, are called n
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Bupivacaine is one of the local anesthetics commonly
2021-09-15
Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root Pam3CSK4 (DRG) neurons [5], [6], [7],
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The stress of accelerated lactate production in cancer
2021-09-15
The stress of accelerated lactate production in cancer adenosine monophosphate is moderated by the overexpression of lactate transporters – symporters for lactate anions and protons called monocarboxylate transporters (MCTs) – that are capable of bidirectional transport depending on the environment
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In summary through medicinal chemistry design and computer a
2021-09-14
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d
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Foreign polypeptide antigens can be
2021-09-14
Foreign polypeptide antigens can be incorporated into VLPs to create “chimeric” structures, either as fusions to either end of the VLP capsid (coat) protein (CP) or as additions to well-presented loops [18]. This kind of direct fusion to the coat is usually good for small peptides, however, larger p
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To shed more light on the binding of benzophenanthridine to
2021-09-14
To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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Glutamate aspartate transporters or excitatory amino acid
2021-09-14
Glutamate-aspartate transporters or excitatory amino Cyanine 5-dUTP receptor transporters (EAATs) are essential for the maintenance of glutamate homeostasis. EAATs are widely distributed in central neurons and glial cells (Danbolt, 2001, Martinez-Lozada et al., 2011). They are driven by Na + and K+
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GHRL effect on appetite is influenced by its dose
2021-09-14
GHRL effect on appetite is influenced by its dose and route of administration, where central or peripheral administration of GHRL at low doses increases feed intake, via acting on orexigenic hypothalamic neurons, and decreases appetite at high doses in chickens (Jonaidi et al., 2012), quails (Shoush
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Some but not all GSIs inhibit
2021-09-14
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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tiotropium bromide In order to ensure that the decrease
2021-09-14
In order to ensure that the decrease in ethanol and morphine intake was not due to a sedative effect of SNAP 37889, locomotor activity and motor learning were assessed through behavioural paradigms. Using the locomotor test, SNAP 37889 did not alter any parameters of locomotion; this lack of sedatio
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