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Discovery of 7-hydroxyaporphines as conformationally restricted ligands for beta-1 and beta-2 adrenergic receptors

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Abstract

A series of (−)-nornuciferidine derivatives was synthesized and the non-natural enantiomer of the aporphine alkaloid was discovered to be a potent β1- and β2-adrenergic receptor ligand that antagonized isoproterenol and procaterol induced cyclic AMP increases from adenylyl cyclase, respectively. Progressive deconstruction of the tetracyclic scaffold to less complex cyclic and acyclic analogues revealed that the conformationally restricted (6a-R,7-R)-7-hydroxyaporphine 2 (AK-2-202) was necessary for efficient receptor binding and antagonism.

Graphical abstract: Discovery of 7-hydroxyaporphines as conformationally restricted ligands for beta-1 and beta-2 adrenergic receptors

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Publication details

The article was received on 31 Dec 2017, accepted on 05 Jan 2018 and first published on 22 Jan 2018


Article type: Research Article
DOI: 10.1039/C7MD00656J
Citation: Med. Chem. Commun., 2018, Advance Article
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    Discovery of 7-hydroxyaporphines as conformationally restricted ligands for beta-1 and beta-2 adrenergic receptors

    A. F. Ku and G. D. Cuny, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C7MD00656J

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