Author/Authors :
Jongwon Lim، نويسنده , , Nicholas Stock، نويسنده , , Richard Pracitto، نويسنده , , Julia K. Boueres، نويسنده , , Benito Munoz، نويسنده , , Ashok Chaudhary، نويسنده , , Angelina M. Santini، نويسنده , , Karia Orr، نويسنده , , Herve Schaffhauser، نويسنده , , Robert E. Bezverkov، نويسنده , , Jayashree Aiyar، نويسنده , , Shankar Venkatraman، نويسنده ,
Abstract :
A series of N-acridin-9-yl-butane-1,4-diamines were found to be high-affinity ligands of the α2δ subunit of voltage gated calcium channels. The SAR studies of butane-1,4-diamine side chain resulted in the identification of compound 10 (IC50=9 nM), which is more potent than gabapentin (IC50=27 nM). Partial saturation of the acridine ring was also pursued and provided a compound with higher binding affinity than 1.
