5‑Amino‑1MQ
Designer methylquinoline NNMT-inhibitor (nicotinamide N-methyltransferase). PRECLINICAL-ONLY – Kraus 2014 Nature (PMID 24622204) NNMT-knockdown obese mouse-model evidence; Neelakantan 2018 (PMID 28425865) first 5-amino-1MQ molecule-design publication. Human trials do NOT exist.
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WHAT IS 5-AMINO-1MQ?
Detailed overview
5-Amino-1MQ (5-amino-1-methylquinolinium) is a designer methylquinoline-scaffold NNMT-inhibitor (nicotinamide N-methyltransferase, EC 2.1.1.1), published in 2018 by the Neelakantan group at Washington University in St. Louis (Curr Top Med Chem PMID 28425865). The NNMT enzyme methylates nicotinamide to N1-methylnicotinamide using S-adenosyl-methionine (SAM) as a methyl donor, with direct impact on tissue energy-metabolism substrate pools. NNMT overexpression is documented in obese white adipose tissue + hepatocyte contexts (Hong 2015 Diabetologia PMID 25972232); it depletes the SAM pool and accumulates 1-methylnicotinamide, decreasing histone methylation and polyamine synthesis – a downstream marker of obesity + insulin-resistance pathophysiology. Kraus 2014 Nature (PMID 24622204) reported NNMT knockdown in obese mouse models producing +30% metabolic-rate elevation + insulin-sensitivity elevation without training. 5-Amino-1MQ attempts to pharmacologically reproduce this knockdown effect with a selective NNMT-binding pocket inhibitor. CRITICAL: HUMAN TRIALS DO NOT EXIST. Since 2022-2023 the research-chemical underground market sells '50-150 mg/cap 5-amino-1MQ' products online, with label-claim discrepancy + HPLC-untested content. PRECLINICAL-ONLY status: human PK, human bioavailability, human efficacy evidence, and human safety window are NOT known. WADA does NOT explicitly list it, but the 'S0 catch-all non-approved substance' category could potentially apply.
Mechanism
NNMT-inhibitor (nicotinamide N-methyltransferase), designer methylquinoline scaffold – preclinical only
Dosing
Preclinical only (mouse 50-200 mg/kg/day PO extrapolated). NO human Rx dose.
Half-life
ESTIMATED ~4-8h (NO human PK data, extrapolated from mouse model)
Onset
Preclinical mouse model: metabolic-rate elevation 2-4 weeks chronic dose – human NOT known
Legal status
FDA never approved; EU EMA never approved; research-chemical underground market only. WADA NOT explicitly listed, but 'S0 catch-all non-approved substance' category may apply.
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 6
- No established human side-effect profile – preclinical-only NNMT inhibitor with no Phase I/II/III human trials, so the full safety window (PK, NOAEL, LD50) is unknown.
- Research-chemical sourcing risk: label-claim discrepancy and HPLC-untested content – the product may contain the wrong dose, contaminants, or a different molecule (25–30% of analogous online products did not match their label).
- Possible gastrointestinal discomfort with oral (capsule) use (nausea, stomach upset), which taking with food or more fluid may ease – not clinically validated, anecdote-level only.
- Theoretical disruption of NAD+/methyl-donor metabolism: NNMT inhibition shifts SAM-pool and cellular NAD+ balance – the long-term metabolic consequence in humans is unknown.
- Unknown hepatic and renal impact: human liver- and kidney-dependent clearance is uncharacterised, so organ burden and accumulation risk cannot be estimated (in preclinical mouse data ALT/AST did not rise significantly, but this does not extrapolate to humans).
- Unknown drug interactions: a presumed overlap exists with agents acting on NAD+/AMPK/metabolic pathways (e.g. nicotinamide riboside, metformin), but no clinical interaction data exist.
Contraindications · 6
- Pregnancy and breastfeeding – absolute contraindication (no reproductive toxicology or teratogenicity data in humans).
- Any human-consumption context in general – preclinical-only agent with no safe human protocol; intended only for in-vitro/animal research use.
- Pre-existing liver disease – relative contraindication (human hepatic clearance is unknown and the burden cannot be estimated).
- Pre-existing kidney disease – relative contraindication (human renal elimination and accumulation risk are unknown).
- Competitive athletes subject to testing – potential sanction under the WADA 'S0 non-approved substance' clause (the agent was never approved by the FDA/EMA); to be avoided.
- Minors – categorically to be avoided (no human safety data; effect on developing metabolism unknown).
Related Performance Compounds
Same therapeutic category
Studies
Related research and clinical findings
Genetic Nicotinamide N-Methyltransferase (Nnmt) Deficiency in Male Mice Improves Insulin Sensitivity in Diet-Induced Obesity.
Brachs S, Polack J, Brachs M, Jahn-Hofmann K, Elvert R, Pfenninger A, Bärenz F, Margerie D, Mai K, Spranger J, Kannt A
Identification of novel Piperazine based bisubstrate inhibitors of human nicotinamide N-methyltransferase (hNNMT) with potent enzyme inhibition.
Harikrishna AS, Kesavan V
Nicotinamide riboside is uniquely and orally bioavailable in mice and humans
Trammell SAJ, Schmidt MS, Weidemann BJ, Redpath P, Jaksch F, Dellinger RW, et al.
Nicotinamide N-methyltransferase: a methyltransferase regulating cellular metabolism through methyl donor balance
Hong S, Moreno-Navarrete JM, Wei X, Kikukawa Y, Tzameli I, Prasad D, Lee Y, Asara JM, Fernandez-Real JM, Maratos-Flier E, Pissios P.
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The information here is for educational and scientific purposes only. Performance-enhancing compounds (AAS, prohormones, stimulants, doping agents) are illegal without prescription in Hungary and most of the EU, and carry serious health and legal risks. WADA bans them in competitive sport. This is NOT a usage guide, and we do not encourage any illegal use. If you do use them, medical supervision and regular bloodwork are ESSENTIAL. Severe endocrine, cardiovascular, hepatic and psychiatric side effects are possible.