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    GB-115 molecular structure

    GB-115

    NootropicsApproved (Russia)

    Also known as: GB115, Rankvilon, N-(6-phenylhexanoyl)glycyl-L-tryptophanamide, N-(1-oxo-6-phenylhexyl)glycyl-L-tryptophanamide, Ph(CH2)5CO-Gly-L-Trp-NH2, CCK-4 retrodipeptide analog

    GB-115 is a synthetic dipeptide, N-(6-phenylhexanoyl)glycyl-L-tryptophan amide, designed at the Zakusov Research Institute of Pharmacology in Moscow. It belongs to a Russian program that builds short peptides as topological analogs of the active fragment of a regulatory peptide, the same approach that produced noopept and dilept.

    Half-Life: Not established in humans; the published rat pharmacokinetic work reported an absolute oral bioavailability of 4.65 percent for the crystalline substance and did not report a terminal half-life (PMID: 18457023)Route: Oral, Intraperitoneal injection (animal studies), Aerosol spray (form sold on the research chemical market)MW: 434.5 g/molCAS: 678996-63-9
    Last reviewed:
    Nootropics
    Category
    Approved (Russia)
    Research Stage

    Overview

    Best Price Available

    Disguised Alpha logo

    Disguised Alpha

    $59.99

    10 mL aerosol spray · nasal_spray

    At A Glance

    Mechanism

    GB-115 was designed as a retro-dipeptide analog of the beta turn of cholecystokinin tetrapeptide and acts as a low-affinity blocker of central cholecystokinin receptors (PMID: 17886432, PMID: 30295186). In mice and rats, activation of cholecystokinin tetrapeptide type 2 receptors

    Half-Life
    Not established in humans; the published rat pharmacokinetic work reported an absolute oral bioavailability of 4.65 percent for the crystalline substance and did not report a terminal half-life (PMID: 18457023)
    Routes
    OralIntraperitoneal injection (animal studies)Aerosol spray (form sold on the research chemical market)
    Potential Benefits
    Anxiolytic effect after oral administration in outbred mice, BALB/c mice and outbred rats in open field and elevated plus maze tests (PMID: 24130989)Antidepressant-like reduction of immobility time in the forced swim test in outbred, BALB/c and C57Bl/6 mice, weaker than amitriptyline (PMID: 21476266)Reduced average daily ethanol consumption and the alcohol deprivation effect in high-emotionality MR rats after 14 days of treatment (PMID: 27590755)Attenuated anxiety during benzodiazepine withdrawal in outbred and inbred rats, with partial normalization of striatal dopamine metabolites (PMID: 22238979)Reduced stress-related behavior and lowered the cortisol to DHEA-S ratio in four male rhesus monkeys under isolation, comparable to phenazepam (PMID: 39847298)Reported anxiolytic effect with improvements in attention parameters and reaction time in 31 patients with generalized anxiety disorder over 21 days (PMID: 31626171)

    Overview

    GB-115 is a synthetic dipeptide, N-(6-phenylhexanoyl)glycyl-L-tryptophan amide, designed at the Zakusov Research Institute of Pharmacology in Moscow. It belongs to a Russian program that builds short peptides as topological analogs of the active fragment of a regulatory peptide, the same approach that produced noopept and dilept. GB-115 is a retro-analog of the beta turn of cholecystokinin tetrapeptide, and conformational work identified a beta II turn as the structure responsible for its activity (PMID: 17886432, PMID: 24397028, PMID: 30295186). The stereochemistry matters. In the original series of analogs, the L-tryptophan compounds were anxiolytic and the D-tryptophan compounds anxiogenic, and GB-115 was selected as the L-tryptophan lead (PMID: 17886432). It acts as a low-affinity blocker of central cholecystokinin receptors. In mice and rats, activating cholecystokinin tetrapeptide type 2 receptors abolished its anti-anxiety effect and the compound prevented cholecystokinin-induced anxiety, while the alpha2 adrenoceptor antagonist yohimbine did not interact with it, which the authors read as a shared pharmacological target with cholecystokinin tetrapeptide (PMID: 23113301). The animal file is broad. Oral administration produced anxiolytic effects in outbred mice, BALB/c mice and outbred rats in open field and elevated plus maze tests (PMID: 24130989), antidepressant-like reduction of immobility in the forced swim test that was weaker than amitriptyline (PMID: 21476266), reduced average daily ethanol consumption and the alcohol deprivation effect in high-emotionality MR rats (PMID: 27590755), and reduced anxiety during benzodiazepine withdrawal in outbred and inbred rats (PMID: 22238979). A repeated theme is that the effect depends on the animal phenotype: strains with a passive response to emotional stress respond differently from active ones (PMID: 12910281). A study in four male rhesus monkeys under individual caging reported reduced stress-related behavior and a lower cortisol to DHEA-S ratio, comparable to phenazepam (PMID: 39847298). Safety and dependence data in animals are more complete than for most compounds sold this way. A preclinical package found no deaths after single oral administration at up to 6000 mg/kg in mice and 3500 mg/kg in rats, no irreversible organ changes over six months of oral administration in rats and rabbits, and no allergenic, immunotoxic or mutagenic activity and no effect on reproduction or offspring development (PMID: 20726348). After 30 days of daily administration to rats, stopping the compound produced no anxiety, aggression or convulsive signs, in contrast to diazepam withdrawal in the same experiment (PMID: 21899090). Oral bioavailability in rats was low at 4.65 percent for the crystalline substance, which is why later work compared micronized and reformulated versions (PMID: 18457023, PMID: 27017703). Human evidence is Russian and mostly unpublished in indexed journals. Thirty-one patients with generalized anxiety disorder were treated for 21 days, an effective daily dose was identified, and the authors described a fast anxiolytic effect with a stimulating component and favorable changes in attention parameters and reaction time (PMID: 31626171). That report does not describe randomization, blinding or a placebo arm in its published abstract. The Russian trial registry records that study as an open phase IIa pilot, followed by a double-blind, randomized, placebo-controlled multicenter trial sponsored by Valenta Pharm from April 2021 to December 2022, and the Russian product label cites two placebo-controlled trials of 168 and 220 patients, none of which is indexed in PubMed. On 29 December 2023 GB-115 was registered in Russia as the prescription tablet Rankvilon for anxiety states in neurasthenia and adjustment disorders. It has no FDA or EMA authorization, and the aerosol spray sold on the research chemical market is not the registered tablet and is a research-use-only compound in the US market.

    Potential Research Fields

    AnxiolyticsCholecystokinin receptor pharmacologyDipeptide drug designAnxiety and depression models

    Chemical Information

    IUPAC Name

    Not yet available

    CAS Number

    678996-63-9

    Molecular Formula

    C25H30N4O3

    Molecular Mass

    434.5 g/mol

    Dosing & Protocols

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    Interactions

    Contraindications

    None established in humans. Mechanism-based: the compound blocks central cholecystokinin receptors (PMID: 23113301), so concurrent drugs acting on that system are an untested interaction. It potentiated morphine analgesia in mice through supraspinal opioid mechanisms (PMID: 18239806), which makes combination with opioids a mechanism-based concern. It also has immunomodulating activity in mice, stimulating macrophage phagocytosis and the humoral immune response (PMID: 19145294), and suppressed an experimental inflammatory response in rodents (PMID: 22235394), neither of which has been characterized in people.

    Research Disclaimer

    This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.

    Best Price

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    🇺🇸US🇪🇺EU🇬🇧UK
    GB-115 aerosol spray, 10 mL nasal_spray 10 mL aerosol spray● In Stock $59.99BEST

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    Vendors Selling GB-115

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    9-Me-BC (9-Methyl-β-carboline)

    NootropicsPreclinical

    9-Methyl--carboline (9-Me-BC) is a synthetic -carboline alkaloid that has drawn nootropic-community interest for a preclinical property that is genuinely unusual among -carbolines: in rodent and cell-culture studies it appears to stimulate the dopaminergic phenotype - raising tyrosine hydroxylase, the number of differentiated dopamine neurons and dopamine content - while also showing neuroprotective, neurorestorative and anti-inflammatory effects, plus in-vitro MAO-A/MAO-B inhibition [PMID:17913302, PMID:20374418, PMID:32285253].

    t½ Not characterized in humans (no pharmacokinetic data). Community/anecdotal only: ~5-25 mg per day, oral. No validated or approved human dose exists.
    6 studiesView Profile

    Aniracetam

    NootropicsApproved (Italy)

    Aniracetam is a pyrrolidinone in the racetam family, developed by Hoffmann-La Roche under the code Ro 13-5057.

    t½ About half an hour for the parent drug in humans. Plasma elimination half-life was 0.47 to 0.49 hours after a single 400 mg oral dose in 20 healthy male volunteers (PMID: 19025058). Aniracetam is extensively metabolized to N-anisoyl-GABA and anisic acid; in six elderly hospitalized patients with cerebrovascular disease and reduced creatinine clearance, metabolite half-life was 4 to 7 times longer than in young volunteers (PMID: 9062694).
    PreclinicalView Profile

    Bemethyl (bemitil)

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    Bemethyl, known in the Russian literature as bemitil and sold in the region under names including Metaprot, Bemactor and Antihot, is 2-ethylthiobenzimidazole, normally handled as the hydrobromide salt.

    t½ Not established in humans; in healthy volunteers given a single 250 mg oral dose of the Metaprot capsule form, peak serum ethylthiobenzimidazole averaged 0.91 microg/mL at about 1.06 h, and no terminal half-life was reported (PMID: 21870773)
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    Bromantane

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    t½ Not characterized in humans. Dihexa was engineered for metabolic stability (resistant to plasma and enzymatic degradation) and blood-brain-barrier penetration; in preclinical work its central procognitive effects appear to outlast its plasma presence. 5 to 40 mg oral per day (anecdotal range; no established human dose)
    1 studiesView Profile

    View Full Dosage Guide →

    Protocols, calculator & safety for GB-115

    Best Price

    Disguised Alpha logo

    Disguised Alpha

    $59.99

    1 vendors · 1 listings

    Research Score

    30

    0 PubMed studies

    Quality Indicators

    Data Completeness

    63%
    Description
    Mechanism of Action
    Chemical Data
    Dosing Protocols
    Safety Profile
    PubMed Studies
    Interactions
    Vendor Listings

    Quick Facts

    Half-Life

    Not established in humans; the published rat pharmacokinetic work reported an absolute oral bioavailability of 4.65 percent for the crystalline substance and did not report a terminal half-life (PMID: 18457023)

    Molecular Weight

    434.5 g/mol

    Administration

    Oral, Intraperitoneal injection (animal studies), Aerosol spray (form sold on the research chemical market)

    CAS Number

    678996-63-9

    Trial Phase

    Approved (Russia)

    0

    Research Disclaimer

    This information is for educational and research purposes only. Not intended as medical advice. Consult a healthcare professional before use.

    Frequently Asked Questions

    What is GB-115 used for in research?

    GB-115 is a synthetic dipeptide, N-(6-phenylhexanoyl)glycyl-L-tryptophan amide, designed at the Zakusov Research Institute of Pharmacology in Moscow. It belongs to a Russian program that builds short peptides as topological analogs of the active fragment of a regulatory peptide, the same approach that produced noopept and dilept. GB-115 is a retro-analog of the beta turn of cholecystokinin tetrapeptide, and conformational work identified a beta II turn as the structure responsible for its activity (PMID: 17886432, PMID: 24397028, PMID: 30295186).

    The stereochemistry matters. In the original series of analogs, the L-tryptophan compounds were anxiolytic and the D-tryptophan compounds anxiogenic, and GB-115 was selected as the L-tryptophan lead (PMID: 17886432). It acts as a low-affinity blocker of central cholecystokinin receptors. In mice and rats, activating cholecystokinin tetrapeptide type 2 receptors abolished its anti-anxiety effect and the compound prevented cholecystokinin-induced anxiety, while the alpha2 adrenoceptor antagonist yohimbine did not interact with it, which the authors read as a shared pharmacological target with cholecystokinin tetrapeptide (PMID: 23113301).

    The animal file is broad. Oral administration produced anxiolytic effects in outbred mice, BALB/c mice and outbred rats in open field and elevated plus maze tests (PMID: 24130989), antidepressant-like reduction of immobility in the forced swim test that was weaker than amitriptyline (PMID: 21476266), reduced average daily ethanol consumption and the alcohol deprivation effect in high-emotionality MR rats (PMID: 27590755), and reduced anxiety during benzodiazepine withdrawal in outbred and inbred rats (PMID: 22238979). A repeated theme is that the effect depends on the animal phenotype: strains with a passive response to emotional stress respond differently from active ones (PMID: 12910281). A study in four male rhesus monkeys under individual caging reported reduced stress-related behavior and a lower cortisol to DHEA-S ratio, comparable to phenazepam (PMID: 39847298).

    Safety and dependence data in animals are more complete than for most compounds sold this way. A preclinical package found no deaths after single oral administration at up to 6000 mg/kg in mice and 3500 mg/kg in rats, no irreversible organ changes over six months of oral administration in rats and rabbits, and no allergenic, immunotoxic or mutagenic activity and no effect on reproduction or offspring development (PMID: 20726348). After 30 days of daily administration to rats, stopping the compound produced no anxiety, aggression or convulsive signs, in contrast to diazepam withdrawal in the same experiment (PMID: 21899090). Oral bioavailability in rats was low at 4.65 percent for the crystalline substance, which is why later work compared micronized and reformulated versions (PMID: 18457023, PMID: 27017703).

    Human evidence is Russian and mostly unpublished in indexed journals. Thirty-one patients with generalized anxiety disorder were treated for 21 days, an effective daily dose was identified, and the authors described a fast anxiolytic effect with a stimulating component and favorable changes in attention parameters and reaction time (PMID: 31626171). That report does not describe randomization, blinding or a placebo arm in its published abstract. The Russian trial registry records that study as an open phase IIa pilot, followed by a double-blind, randomized, placebo-controlled multicenter trial sponsored by Valenta Pharm from April 2021 to December 2022, and the Russian product label cites two placebo-controlled trials of 168 and 220 patients, none of which is indexed in PubMed. On 29 December 2023 GB-115 was registered in Russia as the prescription tablet Rankvilon for anxiety states in neurasthenia and adjustment disorders. It has no FDA or EMA authorization, and the aerosol spray sold on the research chemical market is not the registered tablet and is a research-use-only compound in the US market.

    What forms does GB-115 come in?

    GB-115 is available in nasal_spray form.

    How much does GB-115 cost?

    Prices start at $59.99 across 1 verified vendor.

    How do I compare GB-115 vendors?

    Compare prices, payment methods, shipping, and COA scores across 1 vendor.

    Research Tools

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    View All

    9-Me-BC (9-Methyl-β-carboline)

    NootropicsPreclinical

    9-Methyl--carboline (9-Me-BC) is a synthetic -carboline alkaloid that has drawn nootropic-community interest for a preclinical property that is genuinely unusual among -carbolines: in rodent and cell-culture studies it appears to stimulate the dopaminergic phenotype - raising tyrosine hydroxylase, the number of differentiated dopamine neurons and dopamine content - while also showing neuroprotective, neurorestorative and anti-inflammatory effects, plus in-vitro MAO-A/MAO-B inhibition [PMID:17913302, PMID:20374418, PMID:32285253].

    t½ Not characterized in humans (no pharmacokinetic data). Community/anecdotal only: ~5-25 mg per day, oral. No validated or approved human dose exists.
    6 studiesView Profile

    Aniracetam

    NootropicsApproved (Italy)

    Aniracetam is a pyrrolidinone in the racetam family, developed by Hoffmann-La Roche under the code Ro 13-5057.

    t½ About half an hour for the parent drug in humans. Plasma elimination half-life was 0.47 to 0.49 hours after a single 400 mg oral dose in 20 healthy male volunteers (PMID: 19025058). Aniracetam is extensively metabolized to N-anisoyl-GABA and anisic acid; in six elderly hospitalized patients with cerebrovascular disease and reduced creatinine clearance, metabolite half-life was 4 to 7 times longer than in young volunteers (PMID: 9062694).
    PreclinicalView Profile

    Bemethyl (bemitil)

    NootropicsApproved (Russia)

    Bemethyl, known in the Russian literature as bemitil and sold in the region under names including Metaprot, Bemactor and Antihot, is 2-ethylthiobenzimidazole, normally handled as the hydrobromide salt.

    t½ Not established in humans; in healthy volunteers given a single 250 mg oral dose of the Metaprot capsule form, peak serum ethylthiobenzimidazole averaged 0.91 microg/mL at about 1.06 h, and no terminal half-life was reported (PMID: 21870773)
    PreclinicalView Profile

    Bromantane

    NootropicsRussia Approved

    Bromantane is an atypical psychostimulant and anxiolytic developed in the 1980s at the Zakusov Institute of Pharmacology of the Russian Academy of Medical Sciences, originally created as an adaptogen for Soviet military and elite athletic use and later approved in Russia for the treatment of neurasthenic and asthenic disorders under the trade name Ladasten.

    34 studiesView Profile

    Cyclazodone

    NootropicsPreclinical

    Cyclazodone is the N-cyclopropyl derivative of pemoline, a 4-oxazolidinone stimulant.

    PreclinicalView Profile

    Dihexa

    NootropicsPreclinical

    Dihexa is a synthetic peptide analogue of the angiotensin IV metabolite LVV-hemorphin-7, developed at Washington State University.

    t½ Not characterized in humans. Dihexa was engineered for metabolic stability (resistant to plasma and enzymatic degradation) and blood-brain-barrier penetration; in preclinical work its central procognitive effects appear to outlast its plasma presence. 5 to 40 mg oral per day (anecdotal range; no established human dose)
    1 studiesView Profile

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