AB-CHMINACA

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AB-CHMINACA (N-[(2S)-1-Amino-3-methyl-1-oxobutan-2-yl]-1-(cyclohexylmethyl)indazole-3-carboxamide) is a drug that acts as a potent agonist for the cannabinoid receptors which produces subjective effects somewhat similar to that of cannabis. It was developed by Pfizer and disclosed in a 2009 patent[1] as a potential analgesic medication, but was never pursued for human use. It was first found in US customs seizures in February 2014 as a shipment of a kilogram of the chemical originating from China, and detected in herbal blends from March 2014.[2]

Cannabinoids are commonly smoked or vaporized to achieve a quick onset of effects and rapid offset. Like other cannabinoids, AB-CHMINACA is insoluble in water but dissolves in ethanol and lipids.

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

AB-CHMINACA, or N-[(2S)-1-Amino-3-methyl-1-oxobutan-2-yl]-1-(cyclohexylmethyl)indazole-3-carboxamide, is a synthetic indazole cannabinoid drug as it contains a substituted indazole core. A cyclohexylmethyl group is bound to this indazole core at R1 of the indazole. This indazole is substituted at R3 with a carboxamide group. The terminal amine of this carboxamide is bonded to a substituted propyl chain with an aminocarbonyl group at R1 and a methyl group at R2.

Pharmacology

AB-CHMINACA is a selective CB1 receptor agonist, being approximately 30 times more active at CB1 over CB2. The reported EC50 values are 7.4 ± 1.5nM at CB1 and 232.4 ± 231.2nM at CB2.[3]

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include injury or death.

Physical effects

  • Spontaneous physical sensations - The "body high" of AB-CHMINACA may be described as a warm, soft, pleasurable, all-encompassing 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. At high doses, this can become uncomfortably intense.
  • Sedation - Generally, the effects on the user's energy levels are primarily sedating. This encourages one to relax, and (at higher doses) fall asleep. This can be suppressed by simply forcing oneself to engage in physical activities.
  • 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, AB-CHMINACA causes an increase in appetite[4], 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.[5] 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.[6]
  • Changes in gravity - AB-CHMINACA can cause vertigo with which the environment appears to be spinning or oscillating. At moderate doses, it can spontaneously induce the sensation of falling, which can be overwhelming and uncomfortable.
  • Perception of bodily heaviness or Perception of decreased weight
  • Dehydration- This is known colloquially as "cotton mouth" in popular American and United Kingdom culture.
  • Nausea

Cognitive effects

Visual effects

Auditory effects

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Toxicity and harm potential

The toxicity and long-term health effects of recreational AB-CHMINACA use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because AB-CHMINACA has very little history of human usage. Anecdotal evidence from people who have tried AB-CHMINACA 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 is worth noting that this compound has been linked to multiple hospitalizations and deaths due to its use.[11][12]

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 may increase one's disposition to mental illness and psychosis[13], particularly in vulnerable individuals with risk factors for psychotic illnesses (like a past or family history of schizophrenia).[14][15][16]

As synthetic cannabinoids are active in the milligram range (with below 1mg being a typical dose for AB-CHMINACA), it is important to use proper precautions when dosing 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 cannabinoids, the chronic use of AB-CHMINACA 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 AB-CHMINACA 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). AB-CHMINACA presents cross-tolerance with all cannabinoids, meaning that after the consumption of AB-CHMINACA all cannabinoids will have a reduced effect.

Legal issues

  • United Kingdom - AB-CHMINACA is a class B drug under the third-generation synthetic cannabinoids generic definition, which came into effect on the 14th December 2016 and is illegal to possess, produce, supply, or import. [17]
  • USA: In January 2015, AB-CHMINACA was designated as a Schedule I controlled substance in the United States.[18]
  • China: As of October 2015 AB-CHMINACA is a controlled substance in China.[19]

See also

External links

References

  1. (WO2009106980) INDAZOLE DERIVATIVES (Patentscope) | https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2009106980
  2. Drug and Chemical Evaluation Section, Office of Diversion Control, Drug Enforcement Administration (December 2014). "N-(1-amino-3-methyl-1-oxobutan-2-yl)-1-(cyclohexylmethyl)-1H-indazole-3-carboxamide (AB-CHMINACA), N-(1-amino-3-methyl-1-oxobutan-2-yl)-1-pentyl-1H-indazole-3-carboxamide (AB-PINACA) and[1-(5-fluoropentyl)-1H-indazol-3-yl](naphthalen-1-yl)methanone(THJ-2201) - Background Information and Evaluation of 'Three Factor Analysis' (Factors 4, 5, and 6) for Temporary Scheduling". | https://www.grassley.senate.gov/sites/default/files/news/upload/3-factor%20analysis%20AB-CHMINACA%20AB-PINACA%20THJ2201%2012172014.pdf
  3. Wiley JL, Marusich JA, Lefever TW, et al. AB-CHMINACA, AB-PINACA, and FUBIMINA: Affinity and Potency of Novel Synthetic Cannabinoids in Producing Δ9-Tetrahydrocannabinol–Like Effects in Mice. The Journal of Pharmacology and Experimental Therapeutics. 2015;354(3):328-339. doi:10.1124/jpet.115.225326. | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4538877/
  4. Mechoulam, R. (1984). Cannabinoids as therapeutic agents. Boca Raton, FL: CRC Press. ISBN 0-8493-5772-1.
  5. How Marijuana Works | http://science.howstuffworks.com/marijuana4.htm
  6. How Marijuana Works | http://science.howstuffworks.com/marijuana4.htm
  7. 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
  8. Every-Palmer, S. Synthetic cannabinoid use and psychosis: an explorative study. Journal of Drug and Alcohol Dependence 2011.
  9. “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
  10. 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
  11. Synthetic Cannabinoid–Related Illnesses and Deaths | http://www.nejm.org/doi/full/10.1056/NEJMp1505328
  12. Suicide attempt with a mix of synthetic cannabinoids and synthetic cathinones: Case report of non-fatal intoxication with AB-CHMINACA, AB-FUBINACA, alpha-PHP, alpha-PVP and 4-CMC | http://www.fsijournal.org/article/S0379-0738(16)00037-2/abstract
  13. 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
  14. Every-Palmer, S. Synthetic cannabinoid use and psychosis: an explorative study. Journal of Drug and Alcohol Dependence 2011.
  15. “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
  16. 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
  17. The Misuse of Drugs Act 1971 (Amendment) Order 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2016/1109/made
  18. Federal Register Vol. 80 No. 20, Friday January 30, 2015. "Schedules of Controlled Substances: Temporary Placement of Three Synthetic Cannabinoids Into Schedule I" (GPO.gov) | https://www.gpo.gov/fdsys/pkg/FR-2015-01-30/pdf/2015-01776.pdf
  19. 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