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- Title
Conformational Restriction of Histamine with a Rigid Bicyclo[3.1.0]hexane Scaffold Provided Selective H3 Receptor Ligands.
- Authors
Watanabe, Mizuki; Kobayashi, Takaaki; Ito, Yoshihiko; Yamada, Shizuo; Shuto, Satoshi; Migaud, Marie
- 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 H3 receptor subtype over the H4 receptor subtype. Notably, compound 7 showed potent binding affinity and over 100-fold selectivity for the H3 receptors (Ki = 5.6 nM for H3 and 602 nM for H4). 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.
- Subjects
HISTAMINE; LIGANDS (Biochemistry); BIOMOLECULES; BIOGENIC amines; HEXANE
- Publication
Molecules, 2020, Vol 25, Issue 16, p3562
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules25163562