Identification and synthesis of [1, 2, 4] triazolo [3, 4-a] phthalazine derivatives as high-affinity ligands to the α 2 δ-1 subunit of voltage gated calcium channel

…, J Gunzner, B Wang, R Pracitto, H Schaffhauser…

文献索引：Lebsack, Alec D.; Gunzner, Janet; Wang, Bowei; Pracitto, Richard; Schaffhauser, Herve; Santini, Angelina; Aiyar, Jayashree; Bezverkov, Robert; Munoz, Benito; Liu, Wensheng; Venkatraman, Shankar Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 10 p. 2463 - 2467

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被引用次数: 35

摘要

We have identified and synthesized a series of [1, 2, 4] triazolo [3, 4-a] phthalazine derivatives as high-affinity ligands to α2δ-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 (IC50= 15nM) and (S)-22 (IC50= 30nM). A potent and selective radioligand,[3H]-(S)-22 was also synthesized to demonstrate that this ligand ...