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Introduction Terpenoids also known as isoprenoids constitute
2022-02-21
Introduction Terpenoids, also known as isoprenoids, constitute a large family of natural products comprising at least 22,000 compounds and play diverse and important roles in plants as hormones, phytosynthetic pigments, and electron carriers [1], [2]. In addition, volatilized terpenoids contribute
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Mepivacaine HCl In neurons and neuroendocrine cells the prod
2022-02-21
In neurons and neuroendocrine cells, the productive fusion pathway is thought to initiate with the Munc18-1/Syx1 complex (Ma et al., 2013, Hughson, 2013, Lai et al., 2017). The Munc13-1 MUN domain is able to catalyze opening of Syx1 (the transition from the Munc18-1/Syx1 complex to the SNARE complex
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Fig summarizes the results for
2022-02-21
Fig. 1 summarizes the results for 500 μM concentration of the drugs. Action of histamine is presented for comparison. Both 1-methylhistamine and Nα-methylhistamine strongly potentiated ASIC1a responses. The concentration-dependence of action of Nα-methylhistamine was measured (Fig. 1B). Fitting by H
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As an inflammatory mediator histamine plays a pivotal
2022-02-21
As an inflammatory mediator, histamine plays a pivotal role in nociceptive processes in both the central and peripheral nervous systems (Gemkow et al., 2009; Hough & Rice, 2011; Tiligada et al., 2009). In this respect, the participation of H3Rs in modulating pain, especially neuropathic pain, has at
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In conclusion we demonstrate for the first time
2022-02-21
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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The therapeutic potential of acetate has been advocated by
2022-02-21
The therapeutic potential of acetate has been advocated by research on neurodegenerative disorders such as Canavan's disease (Arun et al., 2010, Mathew et al., 2005), where oral acetate improved motor function in a genetic model of the disorder, and in studies of behavioural phenotypes associated wi
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The replacement of the P butyl urea cap with
2022-02-21
The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P cy
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As a result of the
2022-02-21
As a result of the capability of modulating the dynamic changes and rearrangement of cytoskeletons, the Rho GTPases, in which RhoA, Cdc42 and Rac1 are best-characterized, have been highlighted as significant contributors for orchestrating neuronal development (Duman et al., 2015, Heasman and Ridley,
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In addition to their functional activation of
2022-02-21
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic Fmoc-His(Boc)-OH.CHA synthesis to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent
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Compared to methadone or morphine buprenorphine is a
2022-02-21
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve
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Although side effects as paresthesia due to the application
2022-02-18
Although side effects as paresthesia due to the application of β-alanine are known, a study in 2006 pointed out that there are no clinical (biochemical or hematological) changes after a long-term supplementation with β-alanine. In 2015, the International Society of Sports Nutrition rejected any argu
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Tail group SAR of the imidazole derived
2022-02-18
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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Here we studied the effects
2022-02-18
Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si
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As our earlier study investigated glut mRNA levels in
2022-02-18
As our earlier study investigated glut mRNA levels in response to a protein load contained in a meal and the studies that used glucose and insulin injections did not examine GLUT expression, this study sought to investigate the effects of hyperglycaemia and insulin on mRNA levels in the spiny dogfis
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Overnight mg dexamethasone suppression testing
2022-02-18
Overnight 1-mg dexamethasone suppression testing (DST) of the BclI polymorphism carriers found them to have lower cortisol levels, suggesting an increased sensitivity to GCs with respect to the transrepression effect of cortisol on the POMC gene of the corticotroph pituitary cells [28]. The exact me
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