(R)-T6

(R)-T6 is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) antagonist and quinuclidine-triazole derivative. It was designed based on the structure of the α7-nAChR agonist QND8 to explore the impact of chirality and structural modifications on receptor subtype selectivity. While its enantiomer (S)-T6 selectively targets the α3β4-nAChR subtype, (R)-T6 exhibits high affinity and selectivity for the α7-nAChR subtype. In preclinical studies, (R)-T6 has demonstrated potent, dose-dependent cytotoxic and antiproliferative effects against non-small cell lung cancer (NSCLC) cell lines (such as A549 and H1975) and small cell lung cancer (SCLC) cell lines (such as DMS-53), outperforming reference chemotherapeutics like doxorubicin. It has also been evaluated for its in vitro permeability, cytotoxicity, and cardiac safety (hERG channel binding), showing a favorable safety profile and high potential oral absorption.

Other names

(R)-3-(4-(3-((4-fluorobenzyl)oxy)phenyl)-1H-1,2,3-triazol-1-yl)quinuclidine(R)-T6 quinuclidine-triazoletriazole-quinuclidine T6