Humulone Modulation of GABA_A Receptors and Its Role in Hops Sleep-Promoting Activity.

ABSTRACT: Humulus lupulus L. (hops) is a major constituent of beer. It exhibits neuroactive properties that make it useful as a sleeping aid. These effects are hypothesized to be mediated by an increase in GABA_A receptor function. In the quest to uncover the constituents responsible for the sedative and hypnotic properties of hops, recent evidence revealed that humulone, a prenylated phloroglucinol derivative comprising 35-70% of hops alpha acids, may act as a positive modulator of GABA_A receptors at low micromolar concentrations. This raises the question whether humulone plays a key role in hops pharmacological activity and potentially interacts with other modulators such as ethanol, bringing further enhancement in GABA_A receptor-mediated effects of beer. Her

SUBMITTER: Benkherouf AY 

PROVIDER: S-EPMC7591795 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature