Supplements

The mGlu7 negative allosteric modulator ADX71743 increases wakefulness and reduces REM and NREM sleep in rats.

In freely moving rats, subcutaneous administration of ADX71743 (50, 100, or 150 mg/kg) increased wakefulness by up to 100% and reduced REM sleep by up to 100% and NREM sleep by up to 75% (all P < .05). The drug also delayed NREM and REM sleep onset by nearly 2-fold for 2 hours after dosing, without altering motor activity or body temperature.

Last updated: Jul 7, 2026•0 RCTs•📖 Read as article →

Evidence Score

Evidence Score26/100
Human RCT☆☆☆☆☆
Meta-analysis☆☆☆☆☆
Mechanism★★★★★
Safety★★★★☆
Confidencelow

Study Evidence

Study 1. Negative allosteric modulator of the metabotropic glutamate receptor 7 ADX71743 increases wakefulness, reduces sleep, and alters stress-induced changes in the brain neurotransmitter levels.

observational

Kalinichev M, Gruner JA, Flik G, Heins M, Haddouk H, Royer-Urios I, Bate ST, Poli S, L&#xfc;tjens R · The international journal of neuropsychopharmacology (2026)

Participants: N/A
Duration: 9 hours post-dose
Intervention: Subcutaneous administration of ADX71743 (50, 100, or 150 mg/kg) or vehicle (50% cyclodextrin in water) given 2 hours after lights on.
Outcome: Wakefulness, REM sleep, NREM sleep, sleep onset latency, motor activity, body temperature, and EEG spectral power.
Effect Size: N/A
Population: Freely moving rats implanted with electrodes and telemetry devices.

Result:

PubMed: 42113604DOI: 10.1093/ijnp/pyag025

Mechanism Graph

ADX71743 selectively inhibits mGlu7 receptor activity
↓
Reduced mGlu7 signaling alters sleep-wake regulatory circuits
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Increases wakefulness and suppresses REM and NREM sleep
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Modulates stress-induced neurotransmitter changes (maintains higher vHipp GABA and 5-HT levels)

Limitations

  • ⚠Animal model (rats) limits direct generalizability to humans
  • ⚠No assessment of long-term effects or potential tolerance with repeated dosing

Frequently Asked Questions

What is ADX71743?▼

ADX71743 is a selective negative allosteric modulator (NAM) of the metabotropic glutamate receptor 7 (mGlu7), used in this study to investigate its role in sleep-wake regulation and stress reactivity in rats.

How did ADX71743 affect sleep in rats?▼

ADX71743 increased wakefulness by up to 100% and reduced REM sleep by up to 100% and NREM sleep by up to 75%, with effects lasting for at least 2 hours after dosing.

Did ADX71743 affect neurotransmitter levels?▼

Basal neurotransmitter levels were unchanged, but ADX71743 attenuated stress-induced declines in GABA and 5-HT in the ventral hippocampus, maintaining higher levels compared to vehicle-treated controls.

Is ADX71743 a stimulant?▼

No, ADX71743 did not alter locomotor activity or body temperature, indicating it has no locomotor stimulant or sedative-like effects.

Products

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References

  1. 1.Kalinichev M, Gruner JA, Flik G, Heins M, Haddouk H, Royer-Urios I, Bate ST, Poli S, L&#xfc;tjens R. "Negative allosteric modulator of the metabotropic glutamate receptor 7 ADX71743 increases wakefulness, reduces sleep, and alters stress-induced changes in the brain neurotransmitter levels.." The international journal of neuropsychopharmacology, 2026. PMID: 42113604 DOI: 10.1093/ijnp/pyag025
Disclaimer: This content is for educational purposes only and is not medical advice. Evidence scores reflect the quality and quantity of available research, not clinical recommendations. Always consult a healthcare professional before starting any supplement or intervention.