Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.

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Chen YL, Liston D, Nielsen J, Chapin D, Dunaiskis A, Hedberg K, Ives J, Johnson J Jr, Jones S

Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.

J Med Chem. 1994 Jun 24;37(13):1996-2000.

PubMed ID

8027982 [ View in PubMed

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Abstract

The synthesis of a series of alkylcarbamates of 1,5-methano-2,3,4,5-tetrahydro-1H-2-benzazepin-7-ol is reported. Many of these compounds are potent acetylcholinesterase (AChE) inhibitors. The in vitro AChE inhibition, cholinergic effects, acute toxicity, and elevation of brain acetylcholine levels in vivo of this series of compounds are described. A representative compound, 1d (5.6 mg/kg, po), was able to reverse hemicolinium-3-induced amnesia in the mouse passive avoidance assay.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Physostigmine	Acetylcholinesterase	IC 50 (nM)	128	N/A	N/A	Details