Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives as high-affinity ligands of the alpha(2)delta subunit of voltage-gated calcium channels |
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| Authors: | Hu Tao Stearns Brian A Campbell Brian T Arruda Jeannie M Chen Chixu Aiyar Jayashree Bezverkov Robert E Santini Angelina Schaffhauser Hervé Liu Wensheng Venkatraman Shankar Munoz Benito |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. tao_hu@merck.com |
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| Abstract: | A novel class of 2H-pyrrolo[3,4-c]pyridazine ligands of the alpha (2) delta subunit of voltage-gated calcium channels is described. Compound 4a with high affinity toward alpha (2) delta was identified through structure-activity relationship studies of the lead compound. Tritiated ligand [(3)H]-4b was synthesized to demonstrate that this ligand binds to the same site as Gabapentin toward alpha (2) delta subunit of voltage-gated calcium channels. |
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