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

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, compound 7 showed potent binding affinity and over 100-fold selectivity for the...

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Detalles Bibliográficos
Autores principales: Watanabe, Mizuki, Kobayashi, Takaaki, Ito, Yoshihiko, Yamada, Shizuo, Shuto, Satoshi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7463632/
https://www.ncbi.nlm.nih.gov/pubmed/32764432
http://dx.doi.org/10.3390/molecules25163562