1-(Arylsulfonyl-isoindol-2-yl)piperazines as 5-HT₆R Antagonists: Mechanochemical Synthesis, In Vitro Pharmacological Properties and Glioprotective Activity.

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 that aberrant constitutive and agonist-induced active states are involved in various pathological mechanisms, the development of biased ligands with different functional profiles at specific 5-HT₆R-elicited signaling pathways may provide a novel therapeutic perspective in the field of neurodegenerative and psychiatric diseases. Based on the structure of SB-258585, an inverse agonist at 5-HT₆R-operated Gs and Cdk5 signaling, we designed a series of 1-(arylsulfonyl-isoindol-2-yl)piperazine de

SUBMITTER: Canale V 

PROVIDER: S-EPMC9855333 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature