2-Phenyl-1H-pyrrole-3-carboxamide as a New Scaffold for Developing 5-HT6 Receptor Inverse Agonists with Cognition-Enhancing Activity
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DOI: 10.1021/acschemneuro.1c00061
Abstract: Serotonin type 6 receptor (5-HT6R) has gained particular interest as a promising target for treating cognitive deficits, given the positive effects of its antagonists in a wide range of memory impairment paradigms. Herein, we report… read more here.
Keywords: cognition enhancing; inverse agonists; phenyl pyrrole; ht6r ... See more keywords
Structural insights into constitutive activity of 5-HT6 receptor.
Sign Up to like & getrecommendations! Published in 2023 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2209917120
Abstract: While most therapeutic research on G-protein-coupled receptors (GPCRs) focuses on receptor activation by (endogenous) agonists, significant therapeutic potential exists through agonist-independent intrinsic constitutive activity that can occur in various physiological and pathophysiological settings. For example,… read more here.
Keywords: insights constitutive; structural insights; constitutive activity; ht6r ... See more keywords
5‐HT6R null mutatrion induces synaptic and cognitive defects
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DOI: 10.1111/acel.13369
Abstract: Serotonin 6 receptor (5‐HT6R) is a promising target for a variety of human diseases, such as Alzheimer's disease (AD) and schizophrenia. However, the detailed mechanism underlying 5‐HT6R activity in the central nervous system (CNS) is… read more here.
Keywords: ht6r null; mutatrion induces; synaptic cognitive; ht6r ... See more keywords
1-(Arylsulfonyl-isoindol-2-yl)piperazines as 5-HT6R Antagonists: Mechanochemical Synthesis, In Vitro Pharmacological Properties and Glioprotective Activity
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DOI: 10.3390/biom13010012
Abstract: In addition to the canonical Gs adenylyl cyclase pathway, the serotonin type 6 receptor (5-HT6R) recruits additional signaling pathways that control cognitive function, brain development, and synaptic plasticity in an agonist-dependent and independent manner. Considering… read more here.
Keywords: ht6r; arylsulfonyl isoindol; activity; piperazines ht6r ... See more keywords