Author/Authors :
Tao Hu، نويسنده , , Brian A. Stearns، نويسنده , , Brian T Campbell، نويسنده , , Jeannie M. Arruda، نويسنده , , Chixu Chen، نويسنده , , Jayashree Aiyar، نويسنده , , Robert E. Bezverkov، نويسنده , , Angelina Santini، نويسنده , , Herve Schaffhauser، نويسنده , , Wensheng Liu، نويسنده , , Shankar Venkatraman، نويسنده , , Benito Munoz، نويسنده ,
Abstract :
A novel class of 2H-pyrrolo[3,4-c]pyridazine ligands of the α2δ subunit of voltage-gated calcium channels is described. Compound 4a with high affinity toward α2δ was identified through structure–activity relationship studies of the lead compound. Tritiated ligand [3H]-4b was synthesized to demonstrate that this ligand binds to the same site as Gabapentin toward α2δ subunit of voltage-gated calcium channels.
Keywords :
Gabapentin , Affinity , SAR.* Corresponding author. Tel.: +1-858-202-5587 , fax: +1-858-202-5752 , e-mail: tao_hu@merck.com
