Synthesis and biological evaluation of 6-aryl-6H-pyrrolo [3, 4-d] pyridazine derivatives as high-affinity ligands of the α 2 δ subunit of voltage-gated calcium channels
…, RE Bezverkov, A Santini, H Schaffhauser…
文献索引：Hu, Tao; Stearns, Brian A.; Campbell, Brian T.; Arruda, Jeannie M.; Chen, Chixu; Aiyar, Jayashree; Bezverkov, Robert E.; Santini, Angelina; Schaffhauser, Herve; Liu, Wensheng; Venkatraman, Shankar; Munoz, Benito Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2031 - 2034
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.
