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ID: ALA1148420
Journal: Bioorg Med Chem Lett
Title: Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel.
Authors: Lebsack AD, Gunzner J, Wang B, Pracitto R, Schaffhauser H, Santini A, Aiyar J, Bezverkov R, Munoz B, Liu W, Venkatraman S.
Abstract: We have identified and synthesized a series of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to alpha 2 delta-1 subunit of voltage gated calcium channels. Structure-activity relationship studies directed toward improving the potency and physical properties of 2 lead to the discovery of 20 (IC(50)=15 nM) and (S)-22 (IC(50)=30 nM). A potent and selective radioligand, [(3)H]-(S)-22 was also synthesized to demonstrate that this ligand binds to the same site as gabapentin.
CiteXplore: 15109633