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The subdivision of HT receptors started in the
2023-08-24

The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)
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Subsequently Palvimaki et al corroborated Ni and Miledi
2023-08-24

Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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Mechanisms implicated in antinociception by A
2023-08-24

Mechanisms implicated in antinociception by A3R agonists in neuropathic pain are summarized in Box 3. Cellular transduction mechanisms for A3Rs include inhibition of cyclic AMP, PKA via Gαi, interactions with PLC/IP3/DAG and signaling via Gαi and Gαq, and interactions with PI3K/MEK/ERK via βγ subuni
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Neural progenitor cells NPCs are self renewing multipotent
2023-08-24

Neural progenitor cells (NPCs) are self-renewing, multipotent cells that are capable of differentiating into neurons, astrocytes and oligodendrocytes. NPCs are activated in response to a variety of pathological states in neurodegenerative diseases such as Parkinson’s disease and multiple sclerosis,
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br Acknowledgments We thank the anonymous reviewers for thei
2023-08-24

Acknowledgments We thank the anonymous reviewers for their constructive comments on the manuscript, and also thank Dr. Hans-U. Dahms for his comments on the manuscript. This work was supported by a grant from the National Research Foundation (2009-0071218) funded to Young-Mi Lee. This work was al
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ppar pathway As also found by Stolarski
2023-08-24

As also found by Stolarski et al. [14], inclusion of N2O in the model is successful in reducing the effect of dynamics [13] in the lower stratosphere in the Northern Hemisphere (30–60°N in our case). The inclusion of N2O also decreased the error bars on the trend values, but the trend values still c
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br Methods br Results From a study population
2023-08-24

Methods Results From a study population of 7069 patients, a total of 149 falls were reported during the study INCB28060 for an incidence rate (IR) of 5.2 falls per 1000 patient-days (PD), 95% confidence interval (CI) 4.4/1000 PD–6.1/1000 PD. The incidence rate ratio (IRR) for patients in the
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The extent to which GPCR oligomerization is a
2023-08-24

The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Having taken a step back from affinity to gain better
2023-08-24

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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In the last decade the zebrafish has
2023-08-24

In the last decade, the zebrafish has emerged as a valuable vertebrate model to systematically dissect the genetic underpinnings of both vertebrate heart development and function [8,9], as well as distinct cardiac diseases such as congenital heart disease [10], cardiomyopathies [11,12] and cardiac a
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In liver the essential organ of lipoprotein synthesis ACL
2023-08-24

In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic U-104 receptor to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important bridge be
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br Materials and methods br Results br Discussion Despite th
2023-08-24

Materials and methods Results Discussion Despite the relative complexity of immunotherapy, such treatment may have an important role, in conjunction with other therapies in the treatment of cancer refractory to conventional treatments alone. Clinical studies have recently shown that adding
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br Author contribution br Acknowledgement br Introduction Si
2023-08-24

Author contribution Acknowledgement Introduction Since the initial finding of Gould et al. [1], showing the loss of dendritic spines in the hippocampus after ovariectomy and its rescue after treatment of the animals with estradiol, a tremendous number of studies have demonstrated a role of
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br Materials and methods br
2023-08-24

Materials and methods Results Discussion The current treatment modalities for colorectal cancer are hampered by various issues such as high acquired resistance, long-term complication with potential of cancer recurrence, severe side-effects and poor therapeutic index [50], [51], [52]. Compl
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eletriptan mg Weak and transient interactions of
2023-08-24

Weak and transient interactions of HMGB proteins in such hit-and-run mechanisms are understandable given that “fluorescence loss in photobleaching” (FLIP) experiments employing GFP-labeled HMGBs have shown that in living cells they are the most mobile of all nuclear proteins [144]. The entire pool o
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