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Betahistine N methyl pyridyl ethylamine is a
2022-01-03
Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 bafilomycin agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for th
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Long term effects of prolonged darkness on specific physiolo
2022-01-03
Long-term effects of prolonged darkness on specific physiological activities were also monitored at different leaf positions. Basically, stomatal conductance and CO2 assimilation were different at various leaf stages and were decreased or inhibited significantly within 24 h in all leaf positions upo
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br Introduction Adipose tissue AT in addition to its
2021-12-31
Introduction Adipose tissue (AT), in addition to its function as fak inhibitor storage, is an important endocrine organ and it secretes adipokines (Ahima, 2006). Adipose tissue is related to different physiological processes such as energy metabolism, insulin sensitivity, and inflammation. One im
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Polyunsaturated fatty acids PUFAs represent
2021-12-31
Polyunsaturated fatty acids (PUFAs) represent a class of lipids that contain two or more carbon double (unsaturated) bonds (CC) and classified as n-3, n-6 and n-9 fatty acids. PUFAs including n-3 such as docosahexaenoic Toremifene synthesis (DHA), eicosapentaenoic acid (EPA) and n-6 such as arachid
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br Phylogenetic analysis of vertebrate receptors for
2021-12-31
Phylogenetic analysis of vertebrate receptors for peptides similar to glucagon Genes for receptors for peptides similar to glucagon and other secretin-like hormones have been identified in a number of vertebrate species (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et
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Genetic disruption or pharmacologic inhibition of the hepati
2021-12-31
Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co
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br Discussion According to the generally accepted notion whi
2021-12-31
Discussion According to the generally accepted notion which originated from the study of ATP-depleted WM-8014 the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and the subsequent entry of Ca2+ thr
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So far several methods have
2021-12-30
So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute Ac-YVAD-CHO slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels or on “dye coupling” experiment
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Galanin was shown to play an important role in
2021-12-30
Galanin was shown to play an important role in pain and pain processing [14] and the involvement of neuropeptides in the development of migraine is well established [[24], [25], [26]], however, so far it has not been examined whether systemic galanin levels correlate with migraine. Therefore, we use
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Isoflurane administration during i t procedures can complica
2021-12-30
Isoflurane administration during i.t. procedures can complicate the interpretation of our results since isoflurane has been shown to have both neuroprotective and neurotoxic effects (Jiang et al., 2017). Isoflurane pretreatment has been implicated as having protective effects in ischemia in animal m
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Regarding IAV types of hemagglutinin and types
2021-12-30
Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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Herein we report the discovery of AM AM
2021-12-30
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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The stability and function of the HIF protein are
2021-12-30
The stability and function of the HIF-1α protein are affected by many post-translational modifications (PTMs), including hydroxylation, acetylation, ubiquitination and SUMOylation [[29], [30], [31]]. It has been shown that HIF-1α stability is regulated by LSD1 [25]; in particular, the Set9 histone m
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In the course of studies leading to the discovery of
2021-12-30
In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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Recently anti tumor or antiviral
2021-12-30
Recently, anti-tumor or antiviral strategies using RNAi for both gene silencing and innate-receptor activation were designed; one mechanism of these strategies is activating the intracellular retinoic acid–inducible gene I protein (RIG-I). 5′-Triphosphate RNA (3p-small interfering RNA [siRNA]) is th
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