Development of Pharmacophore Models for the Important Off-Target 5-HT2B Receptor.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01679
Abstract: Toxicity is a major cause of attrition in the development of pharmaceuticals, and the off-target effects are a frequent contributor. The 5-HT2B receptor agonism is known to be responsible for a variety of safety concerns… read more here.
Keywords: ht2b; pharmacophore models; ht2b receptor; development ... See more keywords
Immunomodulatory capacity of the serotonin receptor 5-HT2B in a subset of human dendritic cells
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DOI: 10.1038/s41598-018-20173-y
Abstract: Serotonin is a monoamine neurotransmitter that signals through a wide array of receptors (5-HT1–7) many of which are also involved in immune processes. Dendritic cells (DCs) are crucial players in immune defense by bridging innate… read more here.
Keywords: immunomodulatory capacity; ht2b; serotonin; dendritic cells ... See more keywords
Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic β-cells
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-52590-y
Abstract: Clinical use of olanzapine frequently causes severe hyperglycemia as an adverse effect. In this study, we elucidated mechanisms by which olanzapine reduced insulin secretion using the hamster pancreatic β-cell line HIT-T15. Reverse transcriptional-PCR analysis revealed… read more here.
Keywords: secretion; insulin secretion; ht2b; pancreatic cells ... See more keywords
176 Serotonin receptor 2b (5-ht2b) modulates cardiomyocyte proliferation by regulating the hippo pathway
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DOI: 10.1136/heartjnl-2017-311726.174
Abstract: Heart failure is one of the leading causes of death worldwide. In part, this is due to the inadequate regenerative capacity of cardiomyocytes post-injury. Modulation of the Hippo signalling pathway in mice has been shown… read more here.
Keywords: proliferation; ht2b; yap; hippo pathway ... See more keywords
Putative role of 5-HT2B receptors in migraine pathophysiology
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DOI: 10.1177/0333102416646760
Abstract: Objective In this review we attempt to characterize the acute and chronic role of 5-HT2B receptors with regard to meningeal nociception in animal experiments and clinical data targeting migraine therapy. Background Migraine is a common… read more here.
Keywords: migraine; role ht2b; ht2b; putative role ... See more keywords
Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT2A and 5-HT2B serotonin receptors
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2023.1101290
Abstract: Certain 4-substituted analogs of 1-(2,5-dimethoxyphenyl)isopropylamine (2,5-DMA) are psychoactive classical hallucinogens or serotonergic psychedelic agents that function as human 5-HT2A (h5-HT2A) serotonin receptor agonists. Activation of a related receptor population, h5-HT2B receptors, has been demonstrated to… read more here.
Keywords: ht2b; ht2a ht2b; affinity; dimethoxyphenyl isopropylamine ... See more keywords