5F-AKB-48 |
| 5F-AKB-48 | |||||||||||||||||||||||||||||
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| The skeletal formula of 5F-AKB-48 | |||||||||||||||||||||||||||||
| Chemical Nomenclature | |||||||||||||||||||||||||||||
| Substitutive name | 5F-AKB-48 | ||||||||||||||||||||||||||||
| Systematic name | N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide | ||||||||||||||||||||||||||||
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| Summary sheet: 5F-AKB-48 |
5F-AKB-48 (5F-APINACA) is a drug that acts as a potent agonist for the CB1 and CB2 cannabinoid receptors[1] which produces subjective effects somewhat similar to that of cannabis with a short duration and an emphasis on intense physical sensations. Its metabolism has been described in the scientific literature.[2][3][4][5] It was first identified in South Korea[6] and is available for sale as a grey area research chemical through online vendors.
Cannabinoids are commonly smoked or vaporized to achieve a quick onset of effects and rapid offset. 5F-AKB-48 is orally active when dissolved in a lipid, which can increase the duration significantly. Like other cannabinoids, it is insoluble in water but dissolves in ethanol and lipids.
There is some concern over the potential toxicity of many synthetic cannabinoids, so it is strongly discouraged to take this substance for extended periods of time or in excessive doses.[7][8]
Contents
Chemistry
5F-AKB-48, or N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide, is a synthetic indazole cannabinoid as it contains a substituted indazole group. This indazole moeity is substituted at R1 with a fluoropentyl chain, a substitution shared with 5F-PB-22. Additionally, the indazole is substituted at R3 with a carboxamide group. This carboxamide group is N-substituted at its terminal amine group with an adamantane group. This group consists of four fused cyclohexane rings in a unique structure called a diamondoid. 5F-AKB-48 is an analog of STS-135 in which the core indole structure is substituted with an indazole base.
Pharmacology
Although this substance has not been formally studied, from analysis of the structure, it is presumed that 5F-AKB-48 has a similar binding profile to that of other cannabinoids and matches many of the in vivo properties of Δ9-THC. However, the role of these interactions and how they result in the cannabinoid high continues to remain elusive.
Subjective effects
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.
Physical effects
- Spontaneous tactile sensations - The "body high" of 5F-AKB-48 can be described as a sharp, uncomfortable, all-encompassing, and electric tingling sensation that spreads over the body after initial ingestion. It maintains a consistent presence that quickly rises with the onset and hits its limit once the peak has been reached before immediately dissipating.
- Motor control loss - This substance causes a partial to moderate suppression of motor control which intensifies proportional to dose, but rarely results in a complete inability to walk and perform basic movements.
- Appetite enhancement - As with many other cannabinoids, 5F-AKB-48 causes an increase in appetite[9], known colloquially as "the munchies" in popular American and United Kingdom culture. Clinical studies and survey data have found that cannabis increases food enjoyment and interest in food.[10] This is thought to be due to the way in which endocannabinoids in the hypothalamus activate cannabinoid receptors that are responsible for maintaining food intake.[11]
- Pain relief - Cannabinoids have been clinically demonstrated to provide pain relief via agonism of cannabinoid receptors CB1 and CB2, which extends to synthetic cannabinoid receptor agonists. [12][13]
- Perception of increased weight or Perception of decreased weight
- Changes in gravity
- Dehydration- This is known colloquially as "cotton mouth" in popular American and United Kingdom culture.
- Vasodilation
Cognitive effects
- Anxiety - In comparison to other cannabinoids, this compound is particularly prone to inducing feelings of anxiety and it should therefore be avoided by people who are particularly prone to this state of mind.
- Paranoia
- Emotion enhancement
- Thought connectivity
- Thought deceleration
- Conceptual thinking
- Mindfulness
- Information processing suppression
- Dream suppression
- Psychosis - The prolonged usage of synthetic cannabinoids may increase one's disposition to psychosis[14], particularly in vulnerable individuals with risk factors for psychotic illnesses (like a past or family history of schizophrenia).[15][16][17]
Auditory effects
Toxicity and harm potential
The toxicity and long-term health effects of recreational 5F-AKB-48 use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because 5F-AKB-48 has very little history of human usage. Anecdotal evidence from people who have tried 5F-AKB-48 within the community suggest that there do not seem to be any negative health effects attributed to simply trying this drug at low to moderate doses by itself and using it sparingly (but nothing can be completely guaranteed). Informal experiments have shown that overdose will cause physical discomfort including heart palpitations, vertigo and sedation at much lower than dangerous doses, usually causing the user to suffer large amounts of anxiety or to fall asleep.
It has often been recommended that those with severe pre-existing mental conditions should not ingest these substances due to the way they strongly increase one's current state of mind and emotions. Also, like THC, prolonged usage of synthetic cannabinoids including 5F-AKB-48 may increase one's disposition to mental illness and psychosis[18], particularly in vulnerable individuals with risk factors for psychotic illnesses (like a past or family history of schizophrenia).[19][20][21]
As the material is active in the milligram range, it is important to remain vigilant when dosing as to avoid a negative experience. It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
As with other synthetic cannibanoids, the chronic use of 5F-AKB-48 can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage.
Tolerance to many of the effects of 5F-AKB-48 develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). 5F-AKB-48 presents cross-tolerance with all cannabinoids, meaning that after the consumption of 5F-AKB-48 all cannabinoids will have a reduced effect.
Legal issues
- Latvia: 5F-AKB-48 is a Schedule I drug.[22]
- Germany: 5F-APINACA is an Anlage II controlled drug in Germany since July 2013.
- China: As of October 2015 5F-APINACA is a controlled substance in China.[23]
- Czech Republic: 5F-APINACA is banned in the Czech Republic.[24]
See also
External links
References
- ↑ AKB48 (APINACA) and 5F-AKB48 (5F-APINACA) | http://deadiversion.usdoj.gov/drug_chem_info/spice/akb48.pdf
- ↑ Simultaneous quantification of 37 synthetic cannabinoid metabolites in human urine by liquid chromatography-tandem mass spectrometry | http://link.springer.com/article/10.1007%2Fs11419-015-0265-x
- ↑ Concentrations of APINACA, 5F-APINACA, UR-144 and its degradant product in blood samples from six impaired drivers compared to previous reported concentrations of other synthetic cannabinoids | https://www.ncbi.nlm.nih.gov/pubmed/25485949
- ↑ Metabolites of 5F-AKB-48, a synthetic cannabinoid receptor agonist, identified in human urine and liver microsomal preparations using liquid chromatography high-resolution mass spectrometry | https://www.ncbi.nlm.nih.gov/pubmed/24802286
- ↑ Pentylindole/Pentylindazole Synthetic Cannabinoids and Their 5-Fluoro Analogs Produce Different Primary Metabolites: Metabolite Profiling for AB-PINACA and 5F-AB-PINACA | https://www.ncbi.nlm.nih.gov/pubmed/25721194
- ↑ Synthetic cannabinoids abused in South Korea: drug identifications by the National Forensic Service from 2009 to June 2013 | http://link.springer.com/article/10.1007/s11419-013-0213-6
- ↑ Rational Cannabinoid Design - From Intoxicant to Chemical Weapon, Blue-Light | http://www.bluelight.org/vb/threads/762639-Rational-Cannabinoid-Design-From-Intoxicant-to-Chemical-Weapon
- ↑ NAPTHALENE IS SO OVER, Hamilton Morris | http://hamiltonmorris.blogspot.co.uk/2010/06/napthalene-is-so-over.html
- ↑ Mechoulam, R. (1984). Cannabinoids as therapeutic agents. Boca Raton, FL: CRC Press. ISBN 0-8493-5772-1.
- ↑ How Marijuana Works | http://science.howstuffworks.com/marijuana4.htm
- ↑ How Marijuana Works | http://science.howstuffworks.com/marijuana4.htm
- ↑ http://onlinelibrary.wiley.com/doi/10.1111/j.1526-4637.2009.00703.x/abstract
- ↑ Cannabinoids for treatment of chronic non-cancer pain; a systematic review of randomized trials | http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2125.2011.03970.x/abstract
- ↑ http://bjp.rcpsych.org/content/184/2/110.short
- ↑ Every-Palmer, S. Synthetic cannabinoid use and psychosis: an explorative study. Journal of Drug and Alcohol Dependence 2011.
- ↑ http://www.sciencedirect.com/science/article/pii/S0736467910008802
- ↑ http://journals.lww.com/pec-online/Abstract/2010/06000/A_Teenager_With_Agitation__Higher_Than_She_Should.16.aspx
- ↑ http://bjp.rcpsych.org/content/184/2/110.short
- ↑ Every-Palmer, S. Synthetic cannabinoid use and psychosis: an explorative study. Journal of Drug and Alcohol Dependence 2011.
- ↑ http://www.sciencedirect.com/science/article/pii/S0736467910008802
- ↑ http://journals.lww.com/pec-online/Abstract/2010/06000/A_Teenager_With_Agitation__Higher_Than_She_Should.16.aspx
- ↑ Noteikumi par Latvijā kontrolējamajām narkotiskajām vielām, psihotropajām vielām un prekursoriem (Indazola-3-karbonilatvasinājumi) | http://likumi.lv/doc.php?id=121086
- ↑ 关于印发《非药用类麻醉药品和精神药品列管办法》的通知 | http://www.sfda.gov.cn/WS01/CL0056/130753.html
- ↑ Látky, o které byl doplněn seznam č. 4 psychotropních látek (příloha č. 4 k nařízení vlády č. 463/2013 Sb.) | http://www.mzcr.cz/Admin/_upload/files/3/Nov%C3%A9%20PL.pdf