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Conformational Restriction of Histamine with a Rigid Bicyclo[3.1.0]hexane Scaffold Provided Selective H(3)Receptor Ligands

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Title: Conformational Restriction of Histamine with a Rigid Bicyclo[3.1.0]hexane Scaffold Provided Selective H(3)Receptor Ligands
Authors: Watanabe, Mizuki Browse this author →KAKEN DB
Kobayashi, Takaaki Browse this author
Ito, Yoshihiko Browse this author
Yamada, Shizuo Browse this author
Shuto, Satoshi Browse this author →KAKEN DB
Keywords: histamine
H(3)receptor
conformational restriction
selective ligands
Issue Date: Aug-2020
Publisher: MDPI
Journal Title: Molecules
Volume: 25
Issue: 16
Start Page: 3562
Publisher DOI: 10.3390/molecules25163562
Abstract: We designed and synthesized conformationally rigid histamine analogues with a bicyclo[3.1.0]hexane scaffold. All the compounds were selectively bound to the H(3)receptor subtype over the H(4)receptor subtype. Notably, compound7showed potent binding affinity and over 100-fold selectivity for the H(3)receptors (K-i= 5.6 nM for H(3)and 602 nM for H-4). These results suggest that the conformationally rigid bicyclo[3.1.0]hexane structure can be a useful scaffold for developing potent ligands selective for the target biomolecules.
Type: article
URI: http://hdl.handle.net/2115/79750
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

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