Aplysamine-1 and related analogs as histamine H3 receptor antagonists |
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| Authors: | Swanson Devin M Wilson Sandy J Boggs Jamin D Xiao Wei Apodaca Richard Barbier Ann J Lovenberg Timothy W Carruthers Nicholas I |
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| Institution: | Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. dswanso1@prdus.jnj.com |
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| Abstract: | Aplysamine-1 (1), a marine natural product, was synthesized and screened for in vitro activity at the human and rat histamine H3 receptors. Aplysamine-1 (1) was found to possess a high binding affinity for the human H3 receptor (Ki = 30+/-4 nM). Synthetic analogs of 1, including des-bromoaplysamine-1 (10) and dimethyl-{2-4-(3-piperidin-1-yl-propoxy)-phenyl]-ethyl}-amine (13), were potent H3 antagonists. |
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