| Literature DB >> 16300945 |
Devin M Swanson1, Sandy J Wilson, Jamin D Boggs, Wei Xiao, Richard Apodaca, Ann J Barbier, Timothy W Lovenberg, Nicholas I Carruthers.
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.Entities:
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Year: 2005 PMID: 16300945 DOI: 10.1016/j.bmcl.2005.11.003
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823