Aplysamine-1 and related analogs as histamine H3 receptor antagonists
| Autor: | Sandy J. Wilson, Timothy W. Lovenberg, Wei Xiao, Richard Apodaca, Swanson Devin M, Nicholas I. Carruthers, Ann J. Barbier, Jamin D. Boggs |
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| Rok vydání: | 2006 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Ligands Biochemistry Structure-Activity Relationship chemistry.chemical_compound Histamine receptor Drug Discovery Animals Humans Receptors Histamine H3 Structure–activity relationship Receptor Molecular Biology Natural product Molecular Structure Chemistry Alkaloid Organic Chemistry Biological activity Rats Tyrosine Molecular Medicine Histamine H3 receptor Histamine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 16:897-900 |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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