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Inhibitors of the G rdos
2021-09-11

Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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Most of the tumors showed relatively higher GalR mRNA
2021-09-11

Most of the tumors showed relatively higher GalR1 mRNA levels than the controls (Fig. 1a, Table 3). However one patient with the lower GalR1 mRNA levels (#12) had, in fact, relatively lower levels of transcript for galanin and the other galanin receptors. Patient #10 and 4 who were also expressing l
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Because FPR is expressed in VSMCs and its role
2021-09-10

Because FPR-1 is expressed in VSMCs and its role in non-hematopoietic cells is still unclear, we questioned whether FPR-1 would have physiological relevance for vascular behavior, in the same way as it does in neutrophils (Ca2+ homeostasis and angiogenic polymerization). First, we tested if FPR-1 i
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gap 27 br Introduction Fructose bisphosphatase FBPase EC
2021-09-10

Introduction Fructose 1,6-bisphosphatase (FBPase; EC 3.1.3.11) catalyses the irreversible reaction of hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate and inorganic phosphate [1]. Genetic and kinetic studies so far have demonstrated that at least two distinct isoenzymes of FBPase e
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Neuropathic pain NP is a
2021-09-10

Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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br Acknowledgments I thank Takeshi Sakaba for critical readi
2021-09-10

Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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br Formation of secretory vesicles and trafficking toward pl
2021-09-10

Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for Idoxuridine off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/Am
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It is apparent from the data in that none of
2021-09-10

It is apparent from the data in that none of the ligands exhibits significant toxicity as determined by the viability of human embryonic kidney (HEK 293) cells at a concentration of 100 μM. It is also apparent from the data in and that a number of the ligands inhibit the HIV-1 IN enzyme. However,
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Fig summarizes the results for M concentration of
2021-09-10

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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Arena Pharmaceutical introduced a biaryl sulfone derivative
2021-09-10

Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Although we showed that RBL H Sc cells
2021-09-10

Although we showed that RBL-2H3 Sc98 mu opioid receptor antagonist took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter fam
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It is difficult however to assure that observed alterations
2021-09-10

It is difficult, however, to assure that observed alterations of pro-oxidant/antioxidant levels within the studied organisms are related directly to heavy metal pollution, rather than to other accompanying environmental stressors. Environmental factors like oxygen partial pressure, temperature, sali
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The isoenzyme hGSTP is an attractive drug target
2021-09-10

The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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Cichlasoma dimerus as most teleost fish species present
2021-09-10

Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most FPH2 species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (González-Martí
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br Results br Discussion br Materials and
2021-09-10

Results Discussion Materials and Methods Introduction Deoxyribonucleic Sodium Aescinate (DNA) is among the most important biopolymers in living organisms alongside carbohydrates and proteins. DNA is a linear polymer consisting of four types of nucleobases, deoxyribose, and phosphate. Th
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