5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): A novel non-nitrogenous ligand for 5-HT2B receptor

Williams, Dwight A.; Zaidi, Saheem A.; Zhang, Yan

doi:10.1016/j.bmcl.2014.02.029

Cited by 17 publications

(26 citation statements)

References 29 publications

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“…126,127 For example, decarboxylation of tryptophan to tryptamine by Clostridium sporogenes induces enterochromaffin cells to release serotonin, which acts on enteric neurons to stimulate gastrointestinal motility. 128,129 Serotonin is also involved in regulating neurogenesis during development 130 but detangling its role in adult neurodegeneration is complicated by the multitude of serotonin receptor subtypes expressed in the mammalian brain. 131 Gut microbes may also trigger neurotransmitter release via Toll-Like Receptor (TLR) signaling on epithelial, immune and neuronal cells.…”

Section: Immune and Neurotransmitter Signalingmentioning

confidence: 99%

Gut microbes and metabolites as modulators of blood-brain barrier integrity and brain health

2019

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The human gastrointestinal (gut) microbiota comprises diverse and dynamic populations of bacteria, archaea, viruses, fungi, and protozoa, coexisting in a mutualistic relationship with the host. When intestinal homeostasis is perturbed, the function of the gastrointestinal tract and other organ systems, including the brain, can be compromised. The gut microbiota is proposed to contribute to blood-brain barrier disruption and the pathogenesis of neurodegenerative diseases. While progress is being made, a better understanding of interactions between gut microbes and host cells, and the impact these have on signaling from gut to brain is now required. In this review, we summarise current evidence of the impact gut microbes and their metabolites have on blood-brain barrier integrity and brain function, and the communication networks between the gastrointestinal tract and brain, which they may modulate. We also discuss the potential of microbiota modulation strategies as therapeutic tools for promoting and restoring brain health.

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Section: Immune and Neurotransmitter Signalingmentioning

confidence: 99%

Gut microbes and metabolites as modulators of blood-brain barrier integrity and brain health

2019

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“…In the current study, high‐throughput screening of compound libraries (IMM, Institute of Material Medica) revealed that compound 4 , belonging to the flavone class, has a significant anti‐H 3 R activity (Figure ). It was the first found that flavones could inhibit H 3 R. The molecular skeleton of flavones is the preferred structure which possess hepatoprotective, anti‐inflammatory, anti‐oxidation, antibiosis, anticancer, antiviral, cardiovascular‐protective, and anticoagulation activities. To increase the flavones inhibitory activity of H 3 R, further optimization and modification based on the structure of compound 4 was conducted to develop new flavone derivatives with potent H 3 R inhibitory activity.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, biological evaluation, and molecular docking of novel flavones as H₃R inhibitors

Wen

Liu

et al. 2017

Chem Biol Drug Des

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“…In order to study the molecular mechanism of the neuroprotective activity of 5hydroxy-2-(2-phenylethyl)chromone (5-HPEC) (23, Figure 7) [138], a natural product isolated from Imperata cylindrical, Williams and colleagues performed a screening campaign against the CNS receptors, transporters and ion channels. The results showed that 5-HPEC is a 5-HT 2B R antagonist, as was verified in radiobinding assays (K i = 2455 nM) and calcium flux functional assays (IC 50 = 8913 nM).…”

Section: Chromone Derivativesmentioning

confidence: 99%

“…Figure 7. Representative chromone derivatives as non-nitrogenous 5-HT 2B R antagonists[138][139][140].…”

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confidence: 99%

Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor

et al. 2021

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Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT2BR) in 1992, significant progress has been made in 5-HT2BR research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-HT2BR. Emerging evidence has suggested that the 5-HT2BR is implicated in the regulation of the cardiovascular system, fibrosis disorders, cancer, the gastrointestinal (GI) tract, and the nervous system. Eight crystal complex structures of the 5-HT2BR bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT2BR antagonists have been discovered and developed, and several of them have advanced to clinical trials. It is expected that the novel 5-HT2BR antagonists with high potency and selectivity will lead to the development of first-in-class drugs in various therapeutic areas.

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5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): A novel non-nitrogenous ligand for 5-HT2B receptor

Cited by 17 publications

References 29 publications

Gut microbes and metabolites as modulators of blood-brain barrier integrity and brain health

Gut microbes and metabolites as modulators of blood-brain barrier integrity and brain health

Design, synthesis, biological evaluation, and molecular docking of novel flavones as H₃R inhibitors

Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor

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5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): A novel non-nitrogenous ligand for 5-HT2B receptor

Cited by 17 publications

References 29 publications

Gut microbes and metabolites as modulators of blood-brain barrier integrity and brain health

Gut microbes and metabolites as modulators of blood-brain barrier integrity and brain health

Design, synthesis, biological evaluation, and molecular docking of novel flavones as H3R inhibitors

Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor

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Design, synthesis, biological evaluation, and molecular docking of novel flavones as H₃R inhibitors