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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