Title of article :
Aplysamine-1 and related analogs as histamine H3 receptor antagonists
Author/Authors :
Devin M. Swanson، نويسنده , , Sandy J. Wilson، نويسنده , , Jamin D. Boggs، نويسنده , , Wei Xiao، نويسنده , , Richard Apodaca، نويسنده , , Ann J. Barbier، نويسنده , , Timothy W. Lovenberg، نويسنده , , Nicholas I. Carruthers، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
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.
Keywords :
H3 ligand , marine natural product , histamine , Histamine H3 receptor , Aplysamine-1 , Histamine H3 receptor antagonists , Neurotransmitter
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
