Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors

[Display omitted] •NDMC was a strong muscarinic M1 receptor agonist.•While clozapine displayed antagonist-like behavior on M1 receptor.•Brain penetration of NDMC might be regulated clozapine’s clinical efficacy.•Compound 8 indicated robust M1 agonism with high brain permeability.•Compound 8 has a po...

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Published inBioorganic & medicinal chemistry letters Vol. 40; p. 127911
Main Authors Watanabe, Hitoshi, Ishida, Kyoji, Yamamoto, Masanori, Nakako, Tomokazu, Horiguchi, Masakuni, Isobe, Yoshiaki
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 15.05.2021
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Summary:[Display omitted] •NDMC was a strong muscarinic M1 receptor agonist.•While clozapine displayed antagonist-like behavior on M1 receptor.•Brain penetration of NDMC might be regulated clozapine’s clinical efficacy.•Compound 8 indicated robust M1 agonism with high brain permeability.•Compound 8 has a potential to clarify clozapine’s M1 hypothesis.
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2021.127911