Drug intelligence / Profile preview

5j

Development stage
Preclinical
Lead developer
Jiangsu Nhwa Pharmaceutical
Modality
Small Molecules
Administration
Intravenous
01

Overview

5j is a designation used for several distinct experimental small molecules, most prominently a fluorine-containing phenyl acetate derivative developed as an ultra-short-acting sedative and hypnotic agent. Supported by Jiangsu Nhwa Pharmaceutical, this compound acts as a positive allosteric modulator of GABAA receptors, specifically the α1β2γ2 subunit configuration, where it potentiates chloride currents. It is designed to offer a rapid recovery profile, with animal studies showing recovery times reduced by over 50% compared to the benchmark AZD3043, allowing for a swift and clear-headed return to consciousness following anesthesia. Additionally, the name 5j refers to a series of dialkyl (4-amino-5H-chromeno[2,3-d]pyrimidin-5-yl)phosphonates synthesized as potential antitumor agents. These molecules have demonstrated in vitro activity against various cancer cell lines, including lung (A549), prostate (DU-145, PC-3), and breast (MCF-7) cancers, and are also investigated for their potential as CNS-active neuroprotective agents.

02

Targets

GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)GABRB2 (GABA-A receptor subunit beta-2)GABRG2 (GABA-A receptor subunit gamma-2)

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