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compound 4d (Shanghai University of Traditional Chinese Medicine)

Development stage
Preclinical
Lead developer
Shanghai University of Traditional Chinese Medicine
Modality
Small Molecules
Administration
Oral
01

Overview

Compound 4d is a novel 3,4-dihydrocoumarin derivative developed by the Shanghai University of Traditional Chinese Medicine and Jiangxi University of Traditional Chinese Medicine. It acts as a highly potent and selective inhibitor of monoamine oxidase-B (MAO-B), with an IC50 value of 0.37 nM and a selectivity index for hMAO-B over hMAO-A exceeding 270,000. It functions as a reversible and competitive inhibitor of the human MAO-B enzyme. Preclinical studies indicate that compound 4d possesses neuroprotective properties, protecting PC12 cells from 6-OHDA and rotenone-induced damage, and can effectively cross the blood-brain barrier. In animal models of Parkinson's disease, such as the MPTP-induced model, oral administration of compound 4d significantly prevented motor deficits. It also demonstrated a favorable safety profile with low acute toxicity in preclinical tests.

Other names
3,4-dihydrocoumarin derivative 4d
02

Targets

MAOB (Monoamine oxidase B)

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