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Cx mimetic peptides short synthetic peptides corresponding t
2022-04-15
Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino parecoxib sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a concent
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The histamine H receptor H
2022-04-15
The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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CCK Octapeptide, non-sulfated australia The measured ROcc va
2022-04-15
The measured ROcc50 values (4.8 and 42 mg/kg, respectively) were lower than those estimated from the mouse free CCK Octapeptide, non-sulfated australia concentrations (0.4 and 9.3 mg/kg for the sigma-1 and histamine H3 receptor, respectively) or rat CSF levels (0.65 and 4.5 mg/kg, respectively). Thi
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br Materials and methods br Results br Discussion Several hi
2022-04-15
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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In conclusion we demonstrate for the first time that
2022-04-15
In conclusion, we demonstrate, for the first time, that histamine plays a key role in regulating astrocyte function and gliotransmitter release, and we now must re-consider the roles of monoamine neurotransmitters in brain function in the context of astrocyte signalling. Further in vivo studies will
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Glutathione transferases EC also referred to as glutathione
2022-04-14
Glutathione transferases (EC 2.5.1.18; also referred to as glutathione S-transferases, GSTs) are ubiquitous and promiscuous enzymes that catalyze various kinds of reactions involving a wide variety of substrates that are toxic and chemically reactive (Angelucci et al., 2005). The primary function of
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GPR is present primarily in
2022-04-14
GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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Recently a G protein coupled receptor GPR
2022-04-14
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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Several studies have shown that regulation of glutamate
2022-04-14
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 upreg
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br Introduction Most organisms require glucose as
2022-04-14
Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members
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Extending time action is another strategy
2022-04-14
Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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Exposure of human and animals
2022-04-14
Exposure of human and animals to MPTP can reproduce all the characteristic motor and non-motor signs of PD, in addition to mimicking the same responses and side effects to drugs used to treat PD [37], [38]. Anatomically, intoxication with MPTP induces the same selective loss of substantia nigra DA n
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Ghrelin is mostly known for
2022-04-14
Ghrelin is mostly known for its orexigenic properties, whereas the role of DAG on feeding is controversial with studies claiming an orexigenic, anorexigenic or no effect (Inhoff et al, 2009, Toshinai et al, 2006). One of these studies was that of Toshinai and colleagues, who found a link between the
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br Introduction Connexins are transmembrane proteins that al
2022-04-14
Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent pevonedistat via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nutrients to the extracell
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br Introduction Stroke is the second cause
2022-04-13
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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