Cognitive

GB-115

Also known as: Ranquilon, N-phenylacetyl-L-prolylglycine ethyl ester

Clinical Trials
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Key Facts: GB-115

Category
Cognitive
FDA Status
Not FDA Approved
Clinical Status
Phase 3 Completed - Anxiety/adjustment disorders, not yet approved outside Russia
Administration
Oral tablets or sublingual
Typical Dose
6 mg daily (2 mg three times daily)
Frequency
2-3 times daily (morning, afternoon, evening)
Duration
21+ days in clinical trials, effects noted by day 7
Also Known As
Ranquilon, N-phenylacetyl-L-prolylglycine ethyl ester

Mechanism of Action

Cholecystokinin (CCK) is a peptide that acts as a neurotransmitter in the brain, and activating its CCK-2 (also called CCK-B) and CCK-1 receptors tends to trigger anxiety and panic-like states. GB-115 works as an antagonist at these cholecystokinin receptors, meaning it occupies the receptor and blocks CCK from setting off that anxiety signaling. In animal work it specifically prevented anxiety provoked by CCK-4, which shares a pharmacological target with GB-115. This CCK-blocking mechanism is the proposed explanation for its calming effect, and it is distinct from the GABA system that classic sedatives act on.

Research Summary

The research record is real but thin and almost entirely from a single Russian group. In rodent studies (rats, BALB/c and C57Bl/6 mice), GB-115 reduced anxiety induced by CCK-4 and by yohimbine, with effects that varied by mouse strain, and it stayed effective after long-term dosing without producing tolerance or a withdrawal syndrome when stopped. Preclinical safety work has also been published. The only human data comes from a small pilot clinical study of 25 patients with generalized anxiety disorder given 6 mg daily for 21 days, where anxiety scores on the Hamilton scale fell substantially and fatigue scores improved. Importantly, that study was a single-arm pilot with no placebo or control group, so it cannot prove the drug caused the improvement. There are no large randomized controlled trials, no Western regulatory approval, and the evidence base remains preliminary.

Trial Progress:Phase III
Pre
I
II
III
IV
FDA

Dosing Information

Human Trials·Human studies conducted, not FDA approved

Typical Dosing

Community experience

Common Dose

6 mg daily (2 mg three times daily)

Range

2-6 mg per day

Frequency

2-3 times daily (morning, afternoon, evening)

CCK-1 receptor antagonist from Russia. Clinical trial data showed 6 mg/day effective for 21-day cycles with cognitive improvements by day 7. Oral or sublingual administration. No sedation or dependency reported. Some users take 2-4 mg as needed for situational use.

Research Dosing

Scientific studies

Doses observed in research studies

Doses from Studies

Duration

21+ days in clinical trials, effects noted by day 7

Administration

Oral tablets or sublingual

Timing & Administration

Best Time to Take

Morning and throughout the day

2-3 times daily for consistent effects

Food Recommendation

With or without food

Why This Timing?

Clinical trials used three times daily dosing (morning, afternoon, evening) for consistent receptor occupancy. Can be taken with or without food.

Possible Side Effects

Not everyone experiences these effects. Individual responses vary based on dosage, duration, and personal factors.

  • Generally well-tolerated
  • Minimal sedation compared to benzodiazepines
  • Headache (rare)
  • Mild gastrointestinal discomfort
  • No reported dependency or withdrawal
  • Limited long-term safety data
  • Not FDA approved

References

Research This Peptide Further

Frequently Asked Questions

What does GB-115 do?

GB-115 is a synthetic dipeptide anxiolytic developed in Russia, chemically the amide of N-phenylhexanoyl-glycyl-L-tryptophan and described as a retro-analogue of cholecystokinin-4. Rather than acting like a benzodiazepine, it blocks cholecystokinin receptors, a different anti-anxiety route. It has been studied in animals and in a small pilot human study, but it is not an approved or widely available medication.

How does GB-115 work?

Cholecystokinin (CCK) is a peptide that acts as a neurotransmitter in the brain, and activating its CCK-2 (also called CCK-B) and CCK-1 receptors tends to trigger anxiety and panic-like states. GB-115 works as an antagonist at these cholecystokinin receptors, meaning it occupies the receptor and blocks CCK from setting off that anxiety signaling. In animal work it specifically prevented anxiety provoked by CCK-4, which shares a pharmacological target with GB-115. This CCK-blocking mechanism is the proposed explanation for its calming effect, and it is distinct from the GABA system that classic sedatives act on.

Is GB-115 FDA approved?

No, GB-115 is not currently FDA approved. Current status: Phase 3 Completed - Anxiety/adjustment disorders, not yet approved outside Russia

What are the side effects of GB-115?

Reported side effects include: Generally well-tolerated, Minimal sedation compared to benzodiazepines, Headache (rare), Mild gastrointestinal discomfort, No reported dependency or withdrawal. Individual responses vary based on dosage, duration, and personal health factors.

What is the typical dose of GB-115?

Community-reported common dose: 6 mg daily (2 mg three times daily) (2-3 times daily (morning, afternoon, evening)). Range: 2-6 mg per day. Administration: Oral tablets or sublingual. Community-reported doses. Not medical advice. Consult healthcare provider.

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