Title of article
Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives as high-affinity ligands of the α2δ subunit of voltage-gated calcium channels
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
2031
To page
2034
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794332
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