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…
Index: 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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Citation Number: 35
Abstract
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 ...
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