STS-135

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Summary sheet: STS-135
STS-135
STS-135.svg
Chemical Nomenclature
Common names STS-135
Substitutive name 5-fluoro-APICA
Systematic name N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indole-3-carboxamide
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.


Smoked
Dosage
Threshold < 0.5 mg
Light 0.5 - 1.5 mg
Common 1.5 - 2 mg
Strong 2 - 4 mg
Heavy > 4 mg
Duration
Total 30 - 60 minutes
Onset 10 - 45 seconds
Come up 10 - 45 minutes
Peak 10 - 30 minutes
Offset 5 - 10 minutes
After effects 15 - 45 minutes










DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.


STS-135 (also called N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indole-3-carboxamide or 5F-APICA) is a drug that acts as a potent agonist for the cannabinoid receptors which produces subjective effects somewhat similar to that of cannabis with a short duration and an emphasis on intense physical sensations. There is very little information regarding the pharmacology of this compound within the scientific literature. Despite this, however, it 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. STS-135 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 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

STS-135, or N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indole-3-carboxamide, is a synthetic cannabinoid drug containing a substituted indole group. This indole moeity is substituted at R1 with a fluoropentyl chain, a substitution shared with 5F-PB-22, THJ-2201, and 5F-AKB48. 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. STS-135 is an analog of 5F-AKB48 in which the core indazole structure is substituted with an indole base.

Pharmacology

Although this substance has not been formally studied, from analysis of the structure, it is presumed that STS-135 has a similar binding profile to that of other cannabinoids and matches many of the in vivo properties of Δ9-THC.

Formal studies have demonstrated that STS-135 acts a potent cannabinoid receptor agonist in vitro with an EC50 of 51 nM for human CB2 receptors and 13 nM for human CB1 receptors.[1] STS-135 produces bradycardia and hypothermia in rats at doses of 1-10 mg/kg, suggesting cannabinoid-like activity.[2] However, the role of these interactions and how they result in the cannabinoid high experience continues to remain elusive.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These 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 of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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    • Spontaneous tactile sensations - The "body high" of STS-135 can be described as a sharp, uncomfortable, all-encompassing, 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, STS-135 causes an increase in appetite[3], 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.[4] 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.[5]
    • 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.[6][7]
    • Perception of bodily heaviness or Perception of bodily lightness
    • Changes in gravity
    • Dehydration- This is known colloquially as "cotton mouth" in popular American and United Kingdom culture.
    • Vasodilation

Cognitive effects
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Auditory effects
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Toxicity and harm potential

Further information: Synthetic cannabinoid § Toxicity and harm potential, and Research chemicals § Toxicity and harm potential

The toxicity and long-term health effects of recreational STS-135 use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because STS-135 has very little history of human usage. Anecdotal evidence from people who have tried STS-135 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 may increase one's disposition to mental illness and psychosis[12], particularly in vulnerable individuals with risk factors for psychotic illnesses (like a past or family history of schizophrenia).[13][14][15]

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.

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 STS-135 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 STS-135 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). STS-135 presents cross-tolerance with all cannabinoids, meaning that after the consumption of STS-135 all cannabinoids will have a reduced effect.

Legal issues

STS-135 was developed to bypass drug prohibition laws which have banned the possession and sale of many synthetic cannabinoids. As such, it remains legal in most of the world. This means that it is not known to be specifically illegal within any country, but people may still be charged for its possession under certain circumstances such as under analogue laws and with intent to sell or consume.

  • United Kingdom - STS-135 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. [16]
  • China - As of October 2015, STS-135 is a controlled substance in China.[17]
  • Germany - On December 13, 2014 STS-135 was added to the controlled substance act ("BtMG"), making it illegal to produce, sell or possess.[18]
  • Latvia - STS-135 is a Schedule I drug.[19]

See also

External links

References

  1. ↑ 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 | http://pubs.acs.org/doi/abs/10.1021/acschemneuro.5b00107
  2. ↑ 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 | http://pubs.acs.org/doi/abs/10.1021/acschemneuro.5b00107
  3. ↑ Mechoulam, R. (1984). Cannabinoids as therapeutic agents. Boca Raton, FL: CRC Press. ISBN 0-8493-5772-1.
  4. ↑ How Marijuana Works | http://science.howstuffworks.com/marijuana4.htm
  5. ↑ How Marijuana Works | http://science.howstuffworks.com/marijuana4.htm
  6. ↑ http://onlinelibrary.wiley.com/doi/10.1111/j.1526-4637.2009.00703.x/abstract
  7. ↑ 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
  8. ↑ 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
  9. ↑ Every-Palmer, S. Synthetic cannabinoid use and psychosis: an explorative study. Journal of Drug and Alcohol Dependence 2011.
  10. ↑ “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
  11. ↑ 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
  12. ↑ 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
  13. ↑ Every-Palmer, S. Synthetic cannabinoid use and psychosis: an explorative study. Journal of Drug and Alcohol Dependence 2011.
  14. ↑ “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
  15. ↑ 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
  16. ↑ The Misuse of Drugs Act 1971 (Amendment) Order 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2016/1109/made
  17. ↑ 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
  18. ↑ Achtundzwanzigste Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften (28. BtMÄndV)| http://www.buzer.de/gesetz/11392/a189949.htm
  19. ↑ Noteikumi par Latvijā kontrolējamajām narkotiskajām vielām, psihotropajām vielām un prekursoriem (Indola-3-karboksamīdi) | http://likumi.lv/doc.php?id=121086
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