IUPAC Name
Quinolin-8-yl 1-(5-fluoropentyl)-1H-indole-3-carboxylate
Current Scheduling Status
Year(s) and type of review / ECDD meetings
Drug Class
Recommendation (from TRS)
Substance identification
Chemically, 5F-PB-22 is Quinolin-8-yl 1-(5-fluoropentyl)-1H-indole-3- carboxylate. It has no stereoisomers.
Previous review
5F-PB-22 has not been previously pre-reviewed or critically reviewed. A direct critical review was proposed based on information brought to WHO’s attention that 5F-PB-22 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
In vitro and in vivo studies indicate that 5F-PB-22 binds to and activates the CB1 receptor, and induces a number of biological responses that are also triggered by THC and other SCRAs. 5F-PB-22 binds to the CB1 receptor and activates it as a full agonist, and does so with greater potency than XLR-11 and THC. It also suppresses locomotor activity and reduces body temperature (typical cannabinoid effects). 5F-PB-22 completely substitutes for the discriminative stimulus effects of THC in rats with a 22-fold greater potency than THC itself.
Dependence potential
No information from controlled, experimental studies evaluating the dependence potential of 5F-PB-22 in laboratory animals is available. There is, however, some indication of dependency in users. Six users of herbal mixtures containing 5F-AKB-48 and 5F-PB-22 reported abstinence-related symptoms including agitation and suicidal and self-harm ideation. The urge to re-dose has also been reported by users.
Actual abuse and/or evidence of likelihood of abuse
Nonclinical studies indicate that 5F-PB-22 has effects predictive of abuse potential associated with SCRAs. It activates CB1 receptors, depresses locomotor activity and decreases core temperature. 5F-PB-22 completely substitutes for the discriminative stimulus effects of THC in rats with a 22-fold greater potency, suggesting it may induce at least some of the subjective effects of THC, and consequently possesses SCRA-like abuse potential.
5F-PB-22 is sold in the form of herbal mixtures designed for smoking. Intoxication with 5F-PB-22 is commonly associated with seizures, cardiac toxicity, agitation and unconsciousness. Several fatal and nonfatal cases of intoxication associated with 5F-PB-22 use have been reported from Europe and North America since 2013. In some cases, 5F-PB-22 was the only drug found in the biological specimens. Several cases of driving under the influence of 5F-PB- 22 have resulted in accidents and injuries since 2012. Seizures of 5F-PB-22 have been reported from many European countries since 2013. Cases of 5F-PB-22 use have also been reported to UNODC’s Early Warning Advisory from about 30 countries since 2013. 5F-PB-22 is a controlled substance in several countries.
Therapeutic usefulness
There are no currently approved therapeutic human or veterinary uses of 5F-PB-22.
Recommendation
5F-PB-22 binds to and activates CB1 receptors, and it induces a number of biological responses that are also triggered by SCRAs and THC. It produces some cannabimimetic effects in laboratory animals, including the suppression of locomotor activity and reduction of core temperature. It also substitutes for the THC discriminative stimulus. Its dependence or abuse potential has yet not been elucidated in controlled, laboratory studies, although there is some indication of dependency in users. Intoxication with 5F-PB-22 is commonly associated with convulsions, cardiac toxicity, agitation and unconsciousness. Several fatal and nonfatal cases of intoxication associated with 5F-PB-22 use have been reported. Seizures of 5F-PB-22 have been reported in many countries, and it is a controlled substance in a number of countries.
The Committee considered that the degree of risk to public health and society associated with the abuse of 5F-PB-22 is substantial. Therapeutic usefulness has not been recorded. It recognized that 5F-PB-22 has similar abuse liability and has similar ill effects to other SCRAs in Schedule II of the UN Convention on Psychotropic Substances of 1971. The Committee considered that there is sufficient evidence that 5F-PB-22 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. The Committee recommended that 5F- PB-22 (Quinolin-8-yl 1-(5-fluoropentyl)-1H-indole-3-carboxylate) be placed in Schedule II under the UN Convention on Psychotropic Substances of 1971.
Chemically, 5F-PB-22 is Quinolin-8-yl 1-(5-fluoropentyl)-1H-indole-3- carboxylate. It has no stereoisomers.
Previous review
5F-PB-22 has not been previously pre-reviewed or critically reviewed. A direct critical review was proposed based on information brought to WHO’s attention that 5F-PB-22 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
In vitro and in vivo studies indicate that 5F-PB-22 binds to and activates the CB1 receptor, and induces a number of biological responses that are also triggered by THC and other SCRAs. 5F-PB-22 binds to the CB1 receptor and activates it as a full agonist, and does so with greater potency than XLR-11 and THC. It also suppresses locomotor activity and reduces body temperature (typical cannabinoid effects). 5F-PB-22 completely substitutes for the discriminative stimulus effects of THC in rats with a 22-fold greater potency than THC itself.
Dependence potential
No information from controlled, experimental studies evaluating the dependence potential of 5F-PB-22 in laboratory animals is available. There is, however, some indication of dependency in users. Six users of herbal mixtures containing 5F-AKB-48 and 5F-PB-22 reported abstinence-related symptoms including agitation and suicidal and self-harm ideation. The urge to re-dose has also been reported by users.
Actual abuse and/or evidence of likelihood of abuse
Nonclinical studies indicate that 5F-PB-22 has effects predictive of abuse potential associated with SCRAs. It activates CB1 receptors, depresses locomotor activity and decreases core temperature. 5F-PB-22 completely substitutes for the discriminative stimulus effects of THC in rats with a 22-fold greater potency, suggesting it may induce at least some of the subjective effects of THC, and consequently possesses SCRA-like abuse potential.
5F-PB-22 is sold in the form of herbal mixtures designed for smoking. Intoxication with 5F-PB-22 is commonly associated with seizures, cardiac toxicity, agitation and unconsciousness. Several fatal and nonfatal cases of intoxication associated with 5F-PB-22 use have been reported from Europe and North America since 2013. In some cases, 5F-PB-22 was the only drug found in the biological specimens. Several cases of driving under the influence of 5F-PB- 22 have resulted in accidents and injuries since 2012. Seizures of 5F-PB-22 have been reported from many European countries since 2013. Cases of 5F-PB-22 use have also been reported to UNODC’s Early Warning Advisory from about 30 countries since 2013. 5F-PB-22 is a controlled substance in several countries.
Therapeutic usefulness
There are no currently approved therapeutic human or veterinary uses of 5F-PB-22.
Recommendation
5F-PB-22 binds to and activates CB1 receptors, and it induces a number of biological responses that are also triggered by SCRAs and THC. It produces some cannabimimetic effects in laboratory animals, including the suppression of locomotor activity and reduction of core temperature. It also substitutes for the THC discriminative stimulus. Its dependence or abuse potential has yet not been elucidated in controlled, laboratory studies, although there is some indication of dependency in users. Intoxication with 5F-PB-22 is commonly associated with convulsions, cardiac toxicity, agitation and unconsciousness. Several fatal and nonfatal cases of intoxication associated with 5F-PB-22 use have been reported. Seizures of 5F-PB-22 have been reported in many countries, and it is a controlled substance in a number of countries.
The Committee considered that the degree of risk to public health and society associated with the abuse of 5F-PB-22 is substantial. Therapeutic usefulness has not been recorded. It recognized that 5F-PB-22 has similar abuse liability and has similar ill effects to other SCRAs in Schedule II of the UN Convention on Psychotropic Substances of 1971. The Committee considered that there is sufficient evidence that 5F-PB-22 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. The Committee recommended that 5F- PB-22 (Quinolin-8-yl 1-(5-fluoropentyl)-1H-indole-3-carboxylate) be placed in Schedule II under the UN Convention on Psychotropic Substances of 1971.
ECDD Recommendation
Inclusion in Schedule II of the 1971 Convention on Psychotropic Substances
Link to full TRS
9789241210188-eng.pdf417.9 KB
MS Questionnaire Report
4.12_5f-pb-22_annex1.pdf266.91 KB