AKB48 (Item No. ISO00060) is a pentyl indazole with structural similarity to JWH 018 adamantyl carboxamide (Item No. 9001193) and STS-
5F-APINACA (5F-AKB-48) is an analogue of APINACA (AKB-48) fluorinated on the terminal
carbon of the pentyl side chain. It belongs to the category of synthetic cannabinoid receptor
agonists (SCRAs), which have affinity for CB1 and CB2 receptors with activation of the former
accounting for the psychoactive effects of these substances. 5F-APINACA is a psychoactive
substance and has effects similar to Δ
-THC, which, in accordance with the Convention on
Psychotropic Substances of 1971, is listed as Schedule I substance.
5F-APINACA binds with nanomolar affinity to CB1 and CB2 receptors (Ki -value of 1.94 and 0.27
nM, respectively), i.e. with a two-fold and 265-fold higher affinity as compared to THC. 5FAPINACA stimulates CB1-induced [35S]GTPγS binding with high potency and efficacy, and at 0.1
mg/kg i.v. it increases dopamine transmission in the nucleus accumbens. 5F-APINACA is mainly
metabolized by hydroxylation and loss of the fluorine from the N-pentyl side chain.
Detailed information on the toxic effects of 5F-APINACA is not available. In general, SCRAs
may produce nausea, vomiting, agitation, hallucinations, panic attacks, tachycardia, hypertension,
and occasionally chest pain, acute psychosis, and seizures. Clinical signs of toxicity (chest pain,
tachycardia, hypertension, and agitation) following smoking of 5F-APINACA usually resolve
within 4 to 10 h and may require treatment with benzodiazepines. 5F-APINACA smoking has
been associated with myocardial infarction. One non-fatal case was reported in a young man
following smoking of 5F-APINACA 4 h before the onset of chest pain. Five similar cases were
reported after use of other adamantyl-substituted SCRAs.
Long term use of 5F-APINACA is characterized by loss of appetite, cognitive impairment,
breathlessness, cardiac conditions requiring medication, skin ablations, tooth decay, lethargy,
apathy, tremors and insomnia, which are all exacerbated when attempting to reduce use.
Studies on abuse and dependence potential of 5F-APINACA have not been performed, but users
reported a rapidly developing dependence (tolerance, compulsive re-dosing, craving). A variety of
withdrawal symptoms have been reported, such as chest pains and pressure, tachycardia and
palpitations, ongoing insomnia (for over 3 weeks), anxiety, agitation and paranoia.
No therapeutic or medical use has been described for 5F-APINACA and 5F-APINACA is neither
marketed as medicinal product, nor used for industrial purposes.
For recreational use, herbs containing cannabinoids such as 5F-APINACA are smoked, often