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    Fasoracetam (NS-105) molecular structure

    Fasoracetam (NS-105)

    NootropicsPhase 2

    Also known as: NS-105, NFC-1, AEVI-001, LAM-105, NB-001, Fasoracetam monohydrate, 5-oxo-D-prolinepiperidinamide

    Fasoracetam is a racetam developed by Nippon Shinyaku in Japan under the code NS-105 and taken into clinical development for vascular dementia. That program did not lead to approval anywhere.

    Half-Life: Mean terminal half-life 4.82 hours, range 4.06 to 6.99 hours, after single oral doses in adolescents aged 12 to 17, with the drug excreted for the most part unchanged through the kidneys (PMID: 29339723). After intravenous dosing in animals, elimination half-life was 0.67 hours in rats, 2.1 hours in dogs and 1.3 hours in monkeys, with high systemic availability after oral dosing in all three species (PMID: 10604039).Route: OralMW: 196.25 g/molCAS: 110958-19-5
    Last reviewed:
    Nootropics
    Category
    Phase 2
    Research Stage

    Overview

    Best Price Available

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    Disguised Alpha

    $49.99

    60 capsules · capsule

    At A Glance

    Mechanism

    Fasoracetam acts on metabotropic glutamate receptors and modulates adenylyl cyclase in both directions. In rat cerebrocortical membranes it inhibited forskolin-stimulated cyclic AMP formation through pertussis toxin sensitive G proteins and enhanced cyclic AMP formation after per

    Half-Life
    Mean terminal half-life 4.82 hours, range 4.06 to 6.99 hours, after single oral doses in adolescents aged 12 to 17, with the drug excreted for the most part unchanged through the kidneys (PMID: 29339723). After intravenous dosing in animals, elimination half-life was 0.67 hours in rats, 2.1 hours in dogs and 1.3 hours in monkeys, with high systemic availability after oral dosing in all three species (PMID: 10604039).
    Routes
    Oral
    Potential Benefits
    Reversed memory disruption from scopolamine, nucleus basalis lesion, AF64A, baclofen, cerebral ischemia and electroconvulsive shock in rats (PMID: 10494996)Increased acetylcholine release and high-affinity choline uptake in the cerebral cortex and hippocampus of rats (PMID: 10494996)Reduced immobility in the forced swim test and reversed escape failure in learned helplessness in rats (PMID: 9424016)Improved Clinical Global Impressions improvement and severity scores over five weeks in 30 adolescents with ADHD and metabotropic glutamate receptor network mutations, in an open-label study with a single-blind placebo week (PMID: 29339723)

    Overview

    Fasoracetam is a racetam developed by Nippon Shinyaku in Japan under the code NS-105 and taken into clinical development for vascular dementia. That program did not lead to approval anywhere. The molecule was later licensed and revived in the United States as NFC-1 and then AEVI-001 by Aevi Genomic Medicine, which tested it in children and adolescents with attention deficit hyperactivity disorder selected by genotype, and more recently as NB-001 by Nobias Therapeutics for 22q11.2 deletion syndrome. No regulator has approved it for any indication. Material sold to consumers is a research chemical, usually the monohydrate, and the chemistry values below are for the anhydrous form. The Nippon Shinyaku pharmacology, published between 1997 and 2000, describes a compound acting through metabotropic glutamate receptors rather than through a single ion channel. In rat cerebrocortical membranes, NS-105 inhibited forskolin-stimulated cyclic AMP formation through pertussis toxin sensitive G proteins and enhanced it after pertussis toxin pretreatment, a bidirectional pattern shared with the metabotropic glutamate agonist ACPD and blocked by a metabotropic glutamate antagonist (PMID: 9134967). The same bidirectional effect appeared in cultured mouse cortical neurons (PMID: 9272724), and antisense work assigned the inhibitory arm to group II and group III receptors and the facilitatory arm to group I (PMID: 10633154). Two other effects are reported: repeated dosing increased GABA-B receptor numbers in rat cerebral cortex without changing beta-adrenoceptor or 5-HT2 binding (PMID: 9424016), and NS-105 increased acetylcholine release and high-affinity choline uptake in rat cerebral cortex (PMID: 10494996). In rats, NS-105 reversed memory disruption produced by scopolamine, by lesions of the nucleus basalis magnocellularis, by AF64A, by baclofen, by cerebral ischemia and by electroconvulsive shock (PMID: 10494996). It also reduced immobility in the forced swim test and reversed escape failure in learned helplessness (PMID: 9424016). The human data are thin and mostly open-label. A five-week open-label study with a single-blind placebo week enrolled 30 adolescents aged 12 to 17 who had ADHD and mutations in metabotropic glutamate receptor network genes. Mean Clinical Global Impressions scores improved from 3.79 to 2.33 for improvement and 4.83 to 3.86 for severity, both significant, and adverse event rates during the placebo week did not differ from active weeks (PMID: 29339723). The controlled trials that followed did not confirm this. The ASCEND phase 2 program, run in two parts in children and adolescents with and without the relevant copy number variants, completed in 2018 (NCT03265119; NCT03609619) and posted results show the primary ADHD rating scale endpoint was not met in either part, with placebo numerically ahead in Part A and the drug described as safe and well tolerated. A separate placebo-controlled crossover trial in 37 children and adolescents with 22q11 deletion syndrome completed in 2023 (NCT05290493). Fasoracetam is not approved in any country and is not a controlled substance in the United States. It is a research-use-only compound in the United States market.

    Potential Research Fields

    Metabotropic glutamate signalingADHDCognitive enhancementNootropics

    Chemical Information

    IUPAC Name

    Not yet available

    CAS Number

    110958-19-5

    Molecular Formula

    C10H16N2O2

    Molecular Mass

    196.25 g/mol (anhydrous)

    Dosing & Protocols

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    Interactions

    Contraindications

    No formal contraindications have been established. Fasoracetam is excreted mostly unchanged through the kidneys (PMID: 29339723), so reduced renal function would be expected to raise exposure. In rats, radiolabeled NS-105 transferred into the fetus and into milk after a single oral dose (PMID: 10635441), which is a mechanism-based reason to avoid use in pregnancy and lactation. Repeated administration increased GABA-B receptor numbers in rat cerebral cortex (PMID: 9424016), so the pharmacology of repeated exposure is not the same as that of a single dose.

    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.

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    Aniracetam

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    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).
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    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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    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)
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    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

    Mean terminal half-life 4.82 hours, range 4.06 to 6.99 hours, after single oral doses in adolescents aged 12 to 17, with the drug excreted for the most part unchanged through the kidneys (PMID: 29339723). After intravenous dosing in animals, elimination half-life was 0.67 hours in rats, 2.1 hours in dogs and 1.3 hours in monkeys, with high systemic availability after oral dosing in all three species (PMID: 10604039).

    Molecular Weight

    196.25 g/mol (anhydrous)

    Administration

    Oral

    CAS Number

    110958-19-5

    Trial Phase

    Phase 2

    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 Fasoracetam (NS-105) used for in research?

    Fasoracetam is a racetam developed by Nippon Shinyaku in Japan under the code NS-105 and taken into clinical development for vascular dementia. That program did not lead to approval anywhere. The molecule was later licensed and revived in the United States as NFC-1 and then AEVI-001 by Aevi Genomic Medicine, which tested it in children and adolescents with attention deficit hyperactivity disorder selected by genotype, and more recently as NB-001 by Nobias Therapeutics for 22q11.2 deletion syndrome. No regulator has approved it for any indication. Material sold to consumers is a research chemical, usually the monohydrate, and the chemistry values below are for the anhydrous form.

    The Nippon Shinyaku pharmacology, published between 1997 and 2000, describes a compound acting through metabotropic glutamate receptors rather than through a single ion channel. In rat cerebrocortical membranes, NS-105 inhibited forskolin-stimulated cyclic AMP formation through pertussis toxin sensitive G proteins and enhanced it after pertussis toxin pretreatment, a bidirectional pattern shared with the metabotropic glutamate agonist ACPD and blocked by a metabotropic glutamate antagonist (PMID: 9134967). The same bidirectional effect appeared in cultured mouse cortical neurons (PMID: 9272724), and antisense work assigned the inhibitory arm to group II and group III receptors and the facilitatory arm to group I (PMID: 10633154). Two other effects are reported: repeated dosing increased GABA-B receptor numbers in rat cerebral cortex without changing beta-adrenoceptor or 5-HT2 binding (PMID: 9424016), and NS-105 increased acetylcholine release and high-affinity choline uptake in rat cerebral cortex (PMID: 10494996).

    In rats, NS-105 reversed memory disruption produced by scopolamine, by lesions of the nucleus basalis magnocellularis, by AF64A, by baclofen, by cerebral ischemia and by electroconvulsive shock (PMID: 10494996). It also reduced immobility in the forced swim test and reversed escape failure in learned helplessness (PMID: 9424016).

    The human data are thin and mostly open-label. A five-week open-label study with a single-blind placebo week enrolled 30 adolescents aged 12 to 17 who had ADHD and mutations in metabotropic glutamate receptor network genes. Mean Clinical Global Impressions scores improved from 3.79 to 2.33 for improvement and 4.83 to 3.86 for severity, both significant, and adverse event rates during the placebo week did not differ from active weeks (PMID: 29339723). The controlled trials that followed did not confirm this. The ASCEND phase 2 program, run in two parts in children and adolescents with and without the relevant copy number variants, completed in 2018 (NCT03265119; NCT03609619) and posted results show the primary ADHD rating scale endpoint was not met in either part, with placebo numerically ahead in Part A and the drug described as safe and well tolerated. A separate placebo-controlled crossover trial in 37 children and adolescents with 22q11 deletion syndrome completed in 2023 (NCT05290493).

    Fasoracetam is not approved in any country and is not a controlled substance in the United States. It is a research-use-only compound in the United States market.

    What forms does Fasoracetam (NS-105) come in?

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    Research Tools

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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)

    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

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

    PreclinicalView Profile

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    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)
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