Drug intelligence / Profile preview

lupuli flos

Development stage
Phase 3
Lead developer
Medical University Graz
Modality
Small Molecules
Administration
Oral
01

Overview

*Lupuli flos*, the dried female inflorescences of *Humulus lupulus* (hops), is a botanical drug traditionally utilized for its sedative, hypnotic, and anxiolytic properties. In clinical research led by the Medical University of Graz, it has been evaluated as a phytotherapeutic intervention for the management of perioperative anxiety and pain. The pharmacological activity of *Lupuli flos* is attributed to a complex mixture of secondary metabolites, including bitter acids (humulones and lupulones) and prenylated flavonoids (such as xanthohumol). Its primary mechanism of action involves the positive allosteric modulation of GABA-A receptors, facilitating inhibitory neurotransmission. Additionally, components of the extract demonstrate agonist activity at melatonin MT1 and MT2 receptors and antagonist activity at serotonin 5-HT6 and 5-HT7 receptors, which collectively contribute to its sedative and mood-stabilizing effects.

Other names
HopsHumulus lupulusHop strobilesLupuli strobulus
02

Targets

HTR6 (5-hydroxytryptamine receptor 6)HTR7 (5-hydroxytryptamine receptor 7)GABRR (GABA-A receptor subunit rho)MTNR1A (MT1)MTNR1B (Melatonin Receptor 2)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)

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