APICA
Template:Proofread Template:SubstanceBox/2NE1
2NE1 (also known as APICA or JWH-018 adamantyl carboxamide) is a novel synthetic designer cannabinoid. It has been shown to act as a potent agonist for the CB1 and CB2 cannabinoid receptors[1] and has been reported to produce subjective effects somewhat similar to that of cannabis, albeit with a short duration and an emphasis on intense physical sensations.
The name 2NE1 appears to be a reference to the South Korean all-girl K-Pop group.[2] It was first identified in Japan as a constituent of a brown powder sold in late 2011 under the name "Fragrance Powder" as a mixture with its indazole analog AKB48[3] and has since been 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. 2NE1 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. Unlike many novel designer cannabinoids, its metabolism has been described in the scientific literature.[4].
Unlike cannabis, the chronic abuse of synthetic cannabinoids has been associated with multiple deaths and more dangerous side effects and toxicity in general. Therefore, it is strongly discouraged to take this substance for extended periods of time or in excessive doses.
Chemistry
2NE1, or N-(1-adamantyl)-1-pentyl-1H-indole-3-carboxamide, is a synthetic cannabinoid which contains a substituted indole group. This indole moeity is substituted at R1 with a pentyl chain, a substitution shared with JWH-018. Additionally, the indole 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. 2NE1 can be considered the indole analog of AKB48 and the pentyl analog of STS-135.
Pharmacology
Pharmacological studies of 2NE1 report EC50 values of 6.89 ± 0.11nM at CB1 and 7.54 ± 0.11nM at CB2. These values are fairly close to those found for Δ9-THC, although 2NE1 is a full agonist at both receptors, while Δ9-THC is a partial agonist.[5] It is likely that 2NE1 shares 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
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects
- Spontaneous tactile sensations - The "body high" of 2NE1 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, 2NE1 causes an increase in appetite[6], 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.[7] 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.[8]
- 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.[9][10]
- 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[11], particularly in vulnerable individuals with risk factors for psychotic illnesses (like a past or family history of schizophrenia).[12][13][14]
- Increased music appreciation
Auditory effects
Experience reports
Anecdotal reports which describe the effects of this compound within our experience index include:
Additional experience reports can be found here:
Toxicity and harm potential
The toxicity and long-term health effects of recreational 2NE1 use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because 2NE1 has very little history of human usage. Anecdotal evidence from people who have tried 2NE1 within the community suggests 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 2NE1 may increase one's disposition to mental illness and psychosis[15], particularly in vulnerable individuals with risk factors for psychotic illnesses (like a past or family history of schizophrenia).[16][17][18]
As synthetic cannabinoids are active in the milligram range (with below 5mg being a common dose), it is important to use proper precautions when dosing to avoid a negative experience and injury to others.
It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
As with other synthetic cannabinoids, the chronic use of 2NE1 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 2NE1 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). 2NE1 presents cross-tolerance with [[Cross-tolerance::all cannabinoids]], meaning that after the consumption of 2NE all cannabinoids will have a reduced effect.
Legal issues
See also
External links
References
- ↑ Samuel D. Banister, Jordyn Stuart, Richard C. Kevin, Amelia Edington, Mitchell Longworth, Shane M. Wilkinson, Corinne Beinat, Alexandra S. Buchanan, David E. Hibbs, Michelle Glass, Mark Connor, Iain S. McGregor, and Michael Kassiou. "Effects of Bioisosteric Fluorine in Synthetic Cannabinoid Designer Drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135" Chemical Neuroscience. 2015;6(8);1445-1458;doi:10.1021/acschemneuro.5b00107 (Pubmed / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/25921407
- ↑ 2NE1 (Wikipedia) | https://en.wikipedia.org/wiki/2NE1
- ↑ Nahoko Uchiyama, Maiko Kawamura, Ruri Kikura-Hanajiri, Yukihiro Goda. "Identification of two new-type synthetic cannabinoids, N-(1-adamantyl)-1-pentyl-1H-indole-3-carboxamide (APICA) and N-(1-adamantyl)-1-pentyl-1H-indazole-3-carboxamide(APINACA), and detection of five synthetic cannabinoids, AM-1220, AM-2233, AM-1241, CB-13 (CRA-13), and AM-1248, as designer drugs in illegal products" Forensic Toxicol (2012) 30: 114-125;doi:10.1007/s11419-012-0136-7 (SpringerLink) | http://link.springer.com/article/10.1007/s11419-012-0136-7
- ↑ Tim Sobolevsky, Ilya Prasolov and Grigory Rodchenkov. "Study on the phase I metabolism of novel synthetic cannabinoids, APICA and its fluorinated analogue". Drug Testing and Analysis. 2015;7(2);131-142;doi:10.1002/dta.1756 (Pubmed / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/25428705
- ↑ Samuel D. Banister, Jordyn Stuart, Richard C. Kevin, Amelia Edington, Mitchell Longworth, Shane M. Wilkinson, Corinne Beinat, Alexandra S. Buchanan, David E. Hibbs, Michelle Glass, Mark Connor, Iain S. McGregor, and Michael Kassiou. "Effects of Bioisosteric Fluorine in Synthetic Cannabinoid Designer Drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135" Chemical Neuroscience (2015). 6(8). 1445-1458. doi:10.1021/acschemneuro.5b00107
- ↑ 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
- ↑ Causal association between cannabis and psychosis: examination of the evidence - The British Journal of Psychiatry Jan 2004, 184 (2) 110-117 | 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.
- ↑ “Spice” Girls: Synthetic Cannabinoid Intoxication - The Journal of Emergency Medicine Volume 40, Issue 3, March 2011, Pages 296–299 (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0736467910008802
- ↑ A Teenager With Agitation: Higher Than She Should Have Climbed - Pediatric Emergency Care: June 2010 - Volume 26 - Issue 6 - pp 462-465 | http://journals.lww.com/pec-online/Abstract/2010/06000/A_Teenager_With_Agitation__Higher_Than_She_Should.16.aspx
- ↑ Causal association between cannabis and psychosis: examination of the evidence - The British Journal of Psychiatry Jan 2004, 184 (2) 110-117 | 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.
- ↑ “Spice” Girls: Synthetic Cannabinoid Intoxication - The Journal of Emergency Medicine Volume 40, Issue 3, March 2011, Pages 296–299 (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0736467910008802
- ↑ A Teenager With Agitation: Higher Than She Should Have Climbed - Pediatric Emergency Care: June 2010 - Volume 26 - Issue 6 - pp 462-465 | http://journals.lww.com/pec-online/Abstract/2010/06000/A_Teenager_With_Agitation__Higher_Than_She_Should.16.aspx
- ↑ The Misuse of Drugs Act 1971 (Amendment) Order 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2016/1109/made
- ↑ 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