Drug intelligence / Profile preview

imperatorin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal (in Animal Studies)
01

Overview

Imperatorin is a **furocoumarin** phytochemical isolated primarily from plants such as *Angelica dahurica*, *Angelica koreana*, and various citrus fruits[4][8]. It exhibits diverse **pharmacological activities**, including antihypertensive, vasodilatory, antioxidative, antibacterial, anti-parasitic, cognition-enhancing, neuroprotective, anticonvulsant, anticancer, anti-inflammatory, and anti-HIV-1 effects[1][3][4][5]. Mechanistically, imperatorin enhances GABA_A receptor activity, inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), suppresses cyclin D1 to arrest the cell cycle at G1, inhibits voltage-gated sodium channels in neurons, modulates nitric oxide (NO) pathways, increases expression of neurotrophic and antiapoptotic factors such as BDNF and Bcl-2, and modulates the p38/ERK signaling pathway[1][3][4][8]. In animal models and cell lines, imperatorin shows improvement in memory, anxiolytic and anticonvulsant effects, antitumor, and cardioprotective actions, and inhibits HIV-1 replication requiring the transcription factor Sp1[1][3][4][8].

Other names
AmmidinMarmelideMarmelosinPentosalenImperatori8-ISOAMYLENEnoxypsoralenNSC 402949NSC402949NSC-402949AKOS 214-72AKOS214-72AKOS-214-72
02

Targets

GABRR (GABA-A receptor subunit rho)AcetylcholinesteraseButyrylcholinesteraseBACE1 (Beta-site APP-cleaving enzyme 1)ABAT (4-aminobutyrate aminotransferase)

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