Metonitazene: A High-Potency Benzimidazole Opioid for Advanced Pharmacological Research

Product Name: Metonitazene
Chemical Name: N,N-diethyl-2-[(4-methoxyphenyl)methyl]-5-nitro-1H-benzimidazol-1-yl]ethanamine
CAS Number: 14680-51-4
Molecular Formula: C₂₁H₂₇N₅O₃
Molar Mass: 421.52 g/mol
Appearance: Fine, white to off-white crystalline powder or solid

Introduction: A Significant Benzimidazole Opioid for Receptor Studies

Metonitazene is a synthetic compound belonging to the benzimidazole opioid class, a group of chemicals first developed in the 1950s and now of significant interest in modern pharmacological research. It is structurally characterized by a benzimidazole core, a nitro group at the 5-position, and a critical methoxy substitution on the phenyl ring. This specific methoxy modification differentiates it from other compounds in its class, such as Isotonitazene, and is a key factor influencing its receptor binding affinity, potency, and metabolic profile. Metonitazene represents a crucial compound for researchers investigating the intricate structure-activity relationships of synthetic opioids and their profound effects on opioid receptor signaling.

This product is synthesized and provided exclusively as a high-purity chemical for non-human, in vitro research applications conducted by qualified scientific professionals.

Key Characteristics and Research Properties

• Exceptional Potency: Metonitazene is characterized in preclinical literature as an extremely potent and high-efficacy agonist at the μ-opioid receptor (MOR). Its potency is a primary subject of research, with studies indicating it may be significantly more potent than morphine. This high potency demands the use of sophisticated, calibrated analytical equipment and strict handling protocols to ensure researcher safety and experimental accuracy.

• Benzimidazole Class Compound: As a member of the benzimidazole opioid family, its mechanism of action and metabolic pathways are distinct from those of classical opioids like fentanyl or morphine. This makes it a vital tool for comparative pharmacological studies and for expanding the understanding of non-traditional opioid structures.

• Methoxy Substitution: The methoxy group on the phenyl ring is a critical structural feature for SAR studies. This modification influences the compound’s electronic properties, lipophilicity, and its interaction with the opioid receptor binding pocket, affecting both binding affinity and functional activity.

• Receptor Binding Kinetics: This compound is used in vitro to study binding kinetics (e.g., association/dissociation rates, Ki values) and functional efficacy (e.g., EC50, Emax) at human opioid receptor subtypes, providing valuable data on signaling pathways like G-protein activation and beta-arrestin recruitment.

Intended Applications and Research Use

Metonitazene is a chemical for controlled scientific investigation and is categorically not for human or veterinary use.

Its primary applications include, but are not limited to:

• Forensic Toxicology: Used as a high-purity reference standard for the development and validation of analytical methods to detect and quantify this potent substance and its potential metabolites in forensic samples using techniques such as GC-MS, LC-MS/MS, and HPLC-UV.

• Pharmacological Research: In vitro investigation of efficacy, potency, and binding kinetics at human μ-opioid receptors. It is used to study receptor activation, G-protein coupling efficiency, and downstream signaling events.

• Metabolic Pathway Analysis: Investigation of cytochrome P450 metabolism using human liver microsome models to identify characteristic phase I and II metabolites, which is crucial for understanding its metabolic fate and for developing forensic screening protocols.

• Structure-Activity Relationship (SAR) Studies: Essential for researchers mapping how specific molecular modifications on the benzimidazole scaffold—such as the methoxy group—affect binding affinity, efficacy, and selectivity at opioid receptor subtypes, compared to other analogs like Isotonitazene or Etonitazene.

Handling, Storage, and Safety Information

• Purity: >98% (as verified by High-Performance Liquid Chromatography (HPLC) and Mass Spectrometry (MS)).

• Solubility: Soluble in common organic solvents such as dimethyl sulfoxide (DMSO), ethanol, and methanol. It has very limited solubility in water.

• Storage: Must be stored in its original sealed container under inert conditions. Storage should be in a cool, dry, and dark environment, ideally refrigerated between +2°C and +8°C, to protect it from light, moisture, and oxidation, ensuring long-term stability.

• Handling: EXTREME CAUTION – HIGH POTENCY COMPOUND. This material is active in the microgram range and poses a severe risk of life-threatening respiratory depression even through accidental exposure. It must only be handled by trained researchers in a controlled laboratory setting. Mandatory safety protocols include the use of personal protective equipment (PPE) such as nitrile gloves, a lab coat, safety glasses, and the use of a certified fume hood for any manipulation of the pure powder. Proper decontamination procedures must be in place.