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Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors

Szabo, Monika; Lim, Herman D; Herenbrink, Carmen Klein; Christopoulos, Arthur; Lane, J Robert; Capuano, Ben

Authors

Monika Szabo

Herman D Lim

Carmen Klein Herenbrink

Arthur Christopoulos

ROB LANE ROB.LANE@NOTTINGHAM.AC.UK
Associate Professor

Ben Capuano



Abstract

Herein we describe the hybridization of a benzoxazinone M1 scaffold with D2 privileged structures derived from putative and clinically relevant antipsychotics to develop designed multiple ligands. The M1 mAChR is an attractive target for the cognitive deficits in key CNS disorders. Moreover, activity at D2 and 5-HT2A receptors has proven useful for antipsychotic efficacy. We identified 9 which retained functional activity at the target M1 mAChR and D2R and demonstrated high affinity for the 5-HT2AR.

Citation

Szabo, M., Lim, H. D., Herenbrink, C. K., Christopoulos, A., Lane, J. R., & Capuano, B. (2015). Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors. Journal of Medicinal Chemistry, 58(3), 1550-1555. https://doi.org/10.1021/jm5013243

Journal Article Type Article
Acceptance Date Jan 15, 2015
Online Publication Date Jan 30, 2015
Publication Date 2015-02
Deposit Date Apr 22, 2020
Print ISSN 0022-2623
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 58
Issue 3
Pages 1550-1555
DOI https://doi.org/10.1021/jm5013243
Public URL http://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=25590655&retmode=ref&cmd=prlinks
Publisher URL https://pubs.acs.org/doi/10.1021/jm5013243