2024-03-28T10:51:53Zhttps://eprints.lib.hokudai.ac.jp/dspace-oai/requestoai:eprints.lib.hokudai.ac.jp:2115/797502022-11-17T02:08:08Zhdl_2115_20044hdl_2115_124Conformational Restriction of Histamine with a Rigid Bicyclo[3.1.0]hexane Scaffold Provided Selective H(3)Receptor LigandsWatanabe, MizukiKobayashi, TakaakiIto, YoshihikoYamada, ShizuoShuto, SatoshihistamineH(3)receptorconformational restrictionselective ligands460We 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.MDPIJournal Articlehttp://hdl.handle.net/2115/79750Molecules251635622020-08enginfo:doi/10.3390/molecules25163562none