Acryloylfentanyl

Alternative names
Acrylfentanyl
IUPAC Name

N-[(2S)-1-Amino-3-methyl-1-oxobutan-2-yl]-1-pentyl-1H-indazole-3-carboxamide

Year(s) and type of review / ECDD meetings
Drug Class
ECDD Recommendation
Inclusion in Schedule I of the 1961 Convention on Narcotic Drugs
Recommendation (from TRS)
Substance identification
Chemically, acryloylfentanyl is N-Phenyl-N-[1-(2-phenylethyl)piperidin-4-yl] prop-2-enamide. It has no stereoisomers.

Previous review
Acryloylfentanyl has not been previously pre-reviewed or critically reviewed. A direct critical review was proposed based on information brought to WHO’s attention that acryloylfentanyl is clandestinely manufactured, of especially serious risk to public health and society, and of no recognized therapeutic use by any Party. Preliminary information collected from various sources indicated that this substance may cause substantial harm and that it has no medical use.

Similarity to known substances and effects on the central nervous system
Acryloylfentanyl is a μ-opioid receptor agonist with a potency similar to fentanyl. In mice, it produces antinociception and has a longer duration of action than fentanyl. In humans, miosis, decreased consciousness and respiratory depression have been associated with acryloylfentanyl use. These effects were reversed by naloxone.

Dependence potential
No controlled, experimental studies that have investigated the dependence potential of acryloylfentanyl in laboratory animals or humans are available. However, the limited information obtainable from user websites suggests that some users of acryloylfentanyl report an urge to re-dose as well as having symptoms suggestive of withdrawal.

Actual abuse and/or evidence of likelihood of abuse
No controlled, experimental studies that have investigated the abuse potential of acryloylfentanyl in laboratory animals or humans are available. Acryloylfentanyl use has been reported in several European countries and in North America. Data in Europe suggest that the substance is sold online, typically as a powder and as ready-to-use nasal sprays. Acryloylfentanyl is often described as a "research chemical" on such websites. There have been 130 reported deaths associated with acryloylfentanyl use in Europe and North America. Acryloylfentanyl is controlled in a number of countries in different regions of the world.

Therapeutic usefulness
There is no evidence that acryloylfentanyl has been used therapeutically.

Recommendation
The available evidence shows that acryloylfentanyl is an opioid receptor agonist and its pharmacodynamics and clinical effects are similar to those of controlled fentanyls. It binds to opioid receptors and produces antinociception, decreased consciousness, miosis and respiratory depression that can be fatal. The substance has been detected in samples from people who have died and in cases of nonfatal intoxication and its use is a significant concern in a number of countries.

Acryloylfentanyl is a compound liable to similar abuse and with similar ill effects to controlled opioids such as fentanyl, which are included in Schedule I of the Single Convention on Narcotic Drugs of 1961. It has no recorded therapeutic use, and its use has been associated with fatalities. There is sufficient evidence that it is being or is likely to be abused so as to constitute a public health and social problem warranting the placing of the substance under international control. Thus, because it meets the required condition of similarity, it is recommended that acryloylfentanyl (N N-Phenyl-N-[1-(2-phenylethyl)piperidin-4-yl]prop-2- enamide) be placed in Schedule I of the Single Convention on Narcotic Drugs, 1961, as consistent with Article 3, paragraph 3 (iii) of that Convention in that the substance is liable to similar abuse and productive of similar ill effects to drugs in Schedule I.
MS Questionnaire Report