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

• Published in: Bioorganic & medicinal chemistry letters Vol. 40; p. 127911
• Main Authors: Watanabe, Hitoshi, Ishida, Kyoji, Yamamoto, Masanori, Nakako, Tomokazu, Horiguchi, Masakuni, Isobe, Yoshiaki
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15.05.2021

[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...