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Linalool

Clinical trial

Mechanism of Action

Anxiolytic and antispasmodic activity via GABA-A receptor modulation; mild sedative; dominant in sweet basil chemotype
Antimicrobial, antifungal (including Candida albicans), and sedative activity; modulates GABA-A receptors
Positive allosteric modulation of GABA-A receptors (preferential α2/α3 subunit selectivity producing anxiolysis without sedation-tolerance); NMDA glutamate receptor antagonism providing neuroprotective and anticonvulsant effects; 5-HT1A serotonin receptor partial agonism contributing to anxiolytic and antidepressant activity; acetylcholinesterase inhibition potentially relevant to cognitive function; calcium channel blockade producing antispasmodic and antihypertensive effects; anti-inflammatory through NF-κB suppression and COX-2 inhibition.
Linalool, the principal floral terpene of hops lupulin glands, produces anxiolytic, sedative, and anesthetic-sparing effects through multiple CNS mechanisms. It positively modulates GABA-A receptor function in a manner similar to benzodiazepines but at a distinct (potentially TM1-2 transmembrane) binding site, increasing chloride ion conductance in response to GABA. Additionally, linalool antagonizes NMDA glutamate receptors, contributing to antiseizure and neuroprotective effects. Voltage-gated sodium and calcium channels are inhibited by linalool, reducing neuronal excitability. Inhalation of linalool vapor produces rapid CNS distribution via olfactory-limbic pathways, activating GABA-ergic circuits in the amygdala and hypothalamus without the systemic absorption required for oral sedatives.
Modulates GABA-A receptors and voltage-gated calcium channels; reduces glutamate release in cortical synapses

Research Notes

BasilWestern

GABA-A receptor modulation demonstrated in animal models. Anxiolytic effects confirmed in inhalation studies. Antispasmodic activity on smooth muscle documented in vitro.

Clary SageWestern

Antimicrobial activity including anti-Candida effects confirmed in vitro. GABA-A receptor modulation demonstrated in animal models. Sedative effects documented in inhalation studies.

Linalool is extensively studied with multiple mechanisms confirmed in vitro and in vivo. Animal studies consistently demonstrate anxiolytic activity equivalent to diazepam at 1 mg/kg without sedation or motor impairment, attributed to selective GABA-A α2/α3 engagement. NMDA antagonism confirmed in electrophysiological studies with EC50 in the low millimolar range. Anticholinesterase activity validated in kinetic assays. A 2015 human pilot trial of coriander extract demonstrated significant anxiety reduction; larger controlled trials are needed.

HopsWestern

Multiple rodent studies confirm linalool's anxiolytic and sedative activity in elevated plus maze, marble burying, and forced swim tests at inhalation doses achievable in aromatherapy contexts (2.5 µL/L vapor). Linalool inhalation significantly prolonged pentobarbital-induced sleep time and reduced ketamine-induced anesthesia by 30–40% in rodent anesthesia models. A 2018 randomized crossover human study found inhaled linalool reduced salivary cortisol and anxiety scores (STAI) compared to placebo in healthy volunteers undergoing experimental stress, providing first-in-human evidence for the aromatherapy application.

LavenderWestern

Linalool demonstrates anxiolytic activity in multiple clinical trials. The compound inhibits glutamatergic neurotransmission and enhances GABAergic signalling, producing dose-dependent anti-anxiety effects without motor impairment.

Found In 5 Herbs

3D Molecular Structure

Monoterpene Alcohol
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Linalool

Monoterpene AlcoholAromatic plant metabolites with anti-inflammatory properties

Representative pattern: C₁₀H₁₆O

Atoms
Carbon
Oxygen
Hydrogen

Related Compounds (Monoterpene Alcohol)

Live Research

Open on PubMed

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These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease. This content is for educational purposes only and is not a substitute for professional medical advice.