Buy Isotonitazene Powder Online

Isotonitazene is a highly potent synthetic opioid belonging to the 2-benzylbenzimidazole class (nitazenes). It was first synthesized in the 1950s by the pharmaceutical research department of Ciba AG as part of an investigation into structure-activity relationships for analgesic compounds . However, it was never approved for medical use due to its narrow therapeutic window and pronounced risk of respiratory depression . Today, Isotonitazene is exclusively utilized as a certified reference material for analytical and forensic toxicology applications.

This product is classified as a DEA Schedule I controlled substance in the United States  and is listed in Schedule I of the UN Single Convention on Narcotic Drugs .

2. Key Chemical & Physical Properties

• IUPAC Name: N,N-diethyl-2-[2-({4-[(propan-2-yl)oxy]phenyl}methyl)-5-nitro-1H-benzimidazol-1-yl]ethan-1-amine

• Form: Solid powder (freebase); also available as hydrochloride salt

• Melting Point (Hydrochloride): 172–173 °C

• Solubility: Soluble in methanol, chloroform, and DMSO; salts are expected to be sufficiently water-soluble for injectable administration

• LogP (Lipophilicity): 4.85 (calculated)

• Appearance in Seized Samples: Brown, yellow, and white powders; also identified in liquid form

3. Pharmacological Profile

Isotonitazene acts as a highly potent mu-opioid receptor (MOR) agonist and has been characterized as a superagonist .

• Potency: In pre-clinical studies (mice), Isotonitazene demonstrated approximately four times the analgesic potency of fentanyl, with affinity at the mu-opioid receptor approximately 10 times higher than fentanyl .

• Mechanism: It activates Gi-protein signaling pathways and recruits β-arrestin-2 . Isotonitazene exhibits a preference for the G-protein pathway over the β-arrestin-2 pathway, but notably can cause GPCR kinase-independent β-arrestin recruitment .

• Onset & Duration: The drug induces rapid-onset, long-lasting respiratory depression, which is dose-dependent and can be life-threatening even at sub-milligram doses .

• Antagonist: Naloxone blocks Isotonitazene’s activation of the mu-opioid receptor .

4. Regulatory & Legal Status

Due to its high abuse potential and lack of accepted medical use, Isotonitazene is strictly controlled worldwide:

• United States: DEA Schedule I controlled substance. The DEA issued an emergency scheduling order in August 2020, which was made permanent effective December 6, 2021 .

• International: Recommended for Schedule I of the UN Single Convention on Narcotic Drugs (1961) by the WHO Expert Committee on Drug Dependence .

• Germany: Listed in Annex II of the Narcotics Act (BtMG) since May 22, 2021 (verkehrsfähiges, aber nicht verschreibungsfähiges Betäubungsmittel) .

• Canada & UK: Controlled as a benzimidazole-opioid class substance .

Note: Related substances, including N-desethyl isotonitazene (an active metabolite), have also been permanently placed in Schedule I effective January 22, 2026 .

5. Forensic & Research Applications

This product is intended for in vitro laboratory research, forensic analysis, and clinical toxicology only. Not for human or veterinary use.

• Analytical Reference Standard: Used as a certified reference material (CRM) for the identification and quantification of nitazenes in biological matrices (blood, urine) and seized materials .

• LC-MS/MS & GC-MS: Isotonitazene has a detection limit of 0.1 ng/ml and a quantification limit of 0.5 ng/ml using liquid chromatography-mass spectrometry . It is not detected by standard immunoassay-based drug tests .

• Metabolite Identification: Key biomarkers for toxicological testing include:

  • In urine: N- and O-dealkylation products .

  • In blood: 5-Aminoisotonitazene (formed by reduction of the nitro group), which is detected in most blood samples .

  • Active Metabolite: N-Desethyl isotonitazene also exhibits superagonist activity .

• Pharmacological Research: Used to study structure-activity relationships of benzimidazole-opioids, G-protein signaling bias, and mechanisms of opioid-induced respiratory depression .

6. Safety & Hazard Information (GHS)

• Signal Word: Danger

• Hazard Statements:

  • H370: Causes damage to organs

  • H225: Highly Flammable liquid and vapour (for methanolic solutions)

• Precautionary Statements:

  • P260: Do not breathe dust/fume/gas/mist/vapours/spray

  • P264: Wash hands thoroughly after handling

  • P270: Do not eat, drink or smoke when using this product

  • P280: Wear protective gloves/protective clothing/eye protection/face protection

  • P301+P310: IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician

  • P307+P311: IF exposed: call a POISON CENTER or doctor/physician

  • P405: Store locked up

7. Storage & Handling

• Storage Temperature: -20°C (long-term stability ≥ 1 year)

• Formulation: Available as a neat solid or as a 1 mg/ml solution in methanol

• Stability: Stable for at least 1 year when stored at -20°C

Disclaimer: This information is for scientific and educational reference only.