GB-115
Source GB-115 at Peptiology
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Summary
GB‑115 is a synthetic dipeptide that mimics the tetrapeptide cholecystokinin‑4 (CCK‑4). Pre‑clinical studies in mice and rats have shown it to produce anxiolytic effects after oral or intraperitoneal dosing, to stimulate immune functions such as macrophage phagocytosis, and to enhance morphine‑induced analgesia. All evidence comes from animal experiments; no human trials or regulatory approvals have been reported.
Mechanism of Action
GB‑115 acts as a retroanalogue of CCK‑4 and engages the CCK‑4 type‑2 receptor, a pathway implicated in anxiety regulation. In rodents the anxiolytic effect is blocked by CCK‑4‑2 receptor activation, indicating a shared pharmacological target. Additional data suggest it can modulate supraspinal opioid pathways, potentiating morphine analgesia, and it stimulates macrophage activity, reflecting immune‑modulatory actions. Preliminary work in protozoa hints at possible interaction with GABA‑type receptors, but this has not been explored in mammals.
What the Research Shows
A 2008 mouse study reported that GB‑115 (0.1‑10 mg/kg) enhanced peritoneal macrophage phagocytosis and humoral immunity, even reversing cyclophosphamide‑induced immunodeficiency. Behavioural experiments in 2012 showed that the dipeptide prevented CCK‑4‑induced anxiety in C57Bl/6 mice and outbred rats, an effect abolished by CCK‑4‑2 receptor activation, while yohimbine did not alter its action. Oral administration in 2013 produced anxiolysis in outbred mice (0.1‑0.5 mg/kg) and BALB/c mice (0.1‑5 mg/kg), shifting effective doses higher than intraperitoneal routes. A 2007 mouse study found GB‑115 potentiated morphine analgesia in the hot‑plate test via a naloxone‑reversible supraspinal mechanism. A 2023 protozoan assay observed behavioural changes at 10⁻⁷ M, suggesting GABA‑related activity, though relevance to mammals is unclear. No human or clinical data were identified.
Reported Benefits
Animal data indicate that GB‑115 can reduce anxiety‑like behaviour in several rodent strains, with efficacy observed after oral dosing. It also appears to boost innate immune responses, improving macrophage activity and antibody production, and can enhance the analgesic effect of morphine through central opioid mechanisms. These findings suggest potential utility as a non‑sedating anxiolytic, an immunostimulant, or an adjuvant to opioid therapy, pending further research.
Limitations of the Evidence
All reported effects are limited to pre‑clinical rodent models; no human safety or efficacy data exist. The anxiolytic response varies by animal phenotype and strain, indicating possible variability in humans. Dosing ranges differ between oral and intraperitoneal routes, and pharmacokinetic parameters are not described. Potential interactions with opioid or GABA systems remain speculative, and long‑term toxicity has not been assessed.
Safety Considerations
The published abstracts do not report adverse events in the animal studies, but the absence of systematic safety evaluation means toxicity, tolerability, and potential drug interactions are unknown. Caution is warranted regarding possible enhancement of opioid effects and unknown effects on GABAergic pathways. Without human data, any clinical use would be experimental.
How It Is Administered
Studies have employed both oral and intraperitoneal administration in rodents. Oral doses producing anxiolysis ranged from 0.1 to 5 mg/kg, while intraperitoneal doses were effective at 0.1‑10 mg/kg. The dipeptide’s small size and reported stability suggest it can cross biological barriers, but formulation details and bioavailability in humans have not been established.
Routes of Administration
No administration routes recorded yet.
Goals & Uses
No goal associations recorded yet.
Contraindications
No contraindications recorded yet.
Adverse Effects
No adverse effects recorded yet.
Drug Interactions
No drug interactions recorded yet.
Population Constraints
No population constraints recorded yet.
Regulatory Status
No regulatory status recorded yet.
Evidence & Sources
- Journal ArticleLowShipaeva EV, et al.2008-01-01T00:00:00.000000Z
- Journal ArticleLowKolik LG, Gudasheva TA, Seredenin SB2012-01-01T00:00:00.000000Z
- Journal ArticleModerateGudasheva TA, Ostrovskaya RU, Seredenin SB2018-01-01T00:00:00.000000Z
- Journal ArticleLowGruzdev GA, Soboleva LV, Kamensky AA2023-01-01T00:00:00.000000Z
- Journal ArticleLowKolik LG, et al.2013-01-01T00:00:00.000000Z
- Journal ArticleLowKolik LG, Zhukov VN, Seredenin SB2007-01-01T00:00:00.000000Z
Frequently Asked Questions
What type of compound is GB‑115?
GB‑115 is a synthetic dipeptide designed as a retroanalogue of the neuropeptide cholecystokinin‑4, intended to mimic its biological activity while being orally active.
How does GB‑115 reduce anxiety in animal studies?
The dipeptide appears to act on the CCK‑4 type‑2 receptor, a key modulator of anxiety. Blocking this receptor abolishes its anxiolytic effect, indicating that GB‑115’s activity shares a pharmacological target with CCK‑4.
Has GB‑115 been tested in humans?
No. All published data are limited to mouse, rat and protozoan experiments. No clinical trials, safety assessments, or regulatory approvals have been reported.
Can GB‑115 be used together with opioids?
In mice, GB‑115 enhanced morphine‑induced analgesia via a naloxone‑reversible supraspinal mechanism. While this suggests a possible interaction, the relevance to human opioid therapy is unknown and would require careful study.
Is GB‑115 safe for long‑term use?
Safety information is lacking. The abstracts do not describe adverse effects, but systematic toxicity, tolerability, and long‑term impact have not been evaluated in any species.
What is GB-115?
GB‑115 is a synthetic dipeptide that mimics the tetrapeptide cholecystokinin‑4 (CCK‑4). Pre‑clinical studies in mice and rats have shown it to produce anxiolytic effects after oral or intraperitoneal dosing, to stimulate immune functions such as macrophage phagocytosis, and to enhance morphine‑induced analgesia. All evidence comes from animal experiments; no human trials or regulatory approvals have been reported.