U-47700

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Death may occur when opiates are combined with other depressants such as benzodiazepines, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Summary sheet: U-47700
U-47700
U-47700.svg
Chemical Nomenclature
Common names U-47700
Systematic name trans-3,4-dichloro-N-(2-(dimethylamino)cyclohexyl)-N-methylbenzamide
Class Membership
Psychoactive class Opioid
Chemical class Benzamide
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.






Insufflated
Dosage
Threshold 1 - 4 mg
Light 4 - 6 mg
Common 6 - 8 mg
Strong 8 - 10 mg
Heavy 10 mg +
Duration
Total 2 - 3 hours
Onset 5 - 10 minutes
Come up 15 - 20 minutes
Peak 1 - 2 hours
After effects 2 - 4 hours






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.

U-47700[2] is a synthetic opioid substance of the benzamide chemical class that produces analgesic, relaxing, sedating and euphoric effects when administered.

This compound was initially developed by a team at Upjohn in the 1970s.[3] Upjohn created over a dozen patents on related compounds[4][5][6][7][8][9][10][11] until they discovered that U-47700 was the most active.[12] This was done by looking for the key functional groups which gave the greatest activity.[13]

Very little is known about the toxicity of U-47700 and it has very little history of human usage. It is currently available as a gray-area research chemical distributed by online vendors. Many reports suggest that it possesses unique physical properties relative to most opioids such as an unusual amount of causticity (ability to destroy living tissue) that may make it significantly more harmful to expose to the body, particularly when it is injected. It is strongly advised to use harm reduction practices if choosing to use this substance.

Chemistry

U-47700 is an atypical opioid of the benzamide class. It features core phenyl ring with two chlorine atoms at carbons R3 and R4. This ring is connected to an amine group through a carboxyl group (C=O). The terminal nitrogen atom of the amide group is bonded to a methyl carbon and substituted cyclohexane ring. The cyclohexane ring is further substituted at R2 with a dimethylamino group, thus forming the structure of U-47700.

Pharmacology

U-47700 is selective for the µ-opioid receptor, with various sources claiming 7.5x the potency of morphine.[14][15]

Opioids exert their effects by binding to and activating the μ-opioid receptor. This occurs because opioids structurally mimic endogenous endorphins which are naturally found in the body and also work with the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their euphoria, pain relief and anxiolytic effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement.

U-47700 may also be an agonist for the kappa-opioid receptor system. As a result of this, it has become the lead compound of selective kappa-opioid receptor ligands such as U-50488 and U-69,593, which share very similar structures.[16] Its structure led to other chemists experimenting with it to see if rigid analogs would retain activity.[17] Although not used medically, the selective kappa ligands are used in research.[18]

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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Cognitive effects
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After effects
Aftereffects (3).svg

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

U-47700 has a high toxicity relative to its dose due to its extreme potency. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss. It is also potentially lethal when mixed with depressants like alcohol or benzodiazepines.

It is worth noting that U-47700 crystals are particularly corrosive and somewhat caustic to mucous membranes. Careless use may deteriorate the chosen routes of administration so it is important to practice routine maintenance such as soaking the sinus cavity with water prior to and following insufflation. Even if following a regular saline wash of the nasal cavity, multiday use of this substance can create bleeding sores and scabs in the septum and nasal lining. These scabs may persist for days even after all use is ceased. It is unwise to vaporize the substance as it can damage the lungs. Sublingual administration is likely to damage the skin in the mouth.

Combined consumption of U-47700 and fentanyl caused one fatality in Belgium.[20] At least 17 opioid overdoses and several deaths in the USA have also been connected with the use of U-47700.[21]

It is strongly recommended that one use harm reduction practices, and take extreme caution when using this substance.

Tolerance and addiction potential

As with other opioids, the chronic use of U-47700 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 symptoms may occur if a person suddenly stops their usage.

Tolerance to many of the effects of U-47700 develops with prolonged and repeated use. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. 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). U-47700 presents cross-tolerance with all other opioids, meaning that after the consumption of U-47700 all opioids will have a reduced effect.

U-47700 withdrawal symptoms can be especially painful and emerge after 2-4 hours after the last dose administration. It is highly advisable not to become physically dependent on this substance, as physical dependence can develop in a short period.

The risk of fatal opioid overdoses rise sharply after a period of cessation and relapse, largely because of reduced tolerance.[22] To account for this lack of tolerance, it is safer to only dose a fraction of one's usual dosage if relapsing. It has also been found that the environment one is in can play a role in opioid tolerance. In one scientific study, rats with the same history of heroin administration were significantly more likely to die after receiving their dose in an environment not associated with the drug in contrast to a familiar environment.[23]

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

  • Depressants (1,4-Butanediol, 2m2b, alcohol, barbiturates, benzodiazepines, GHB/GBL, methaqualone) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Stimulants - It is dangerous to combine U-47700, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of U-47700, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of U-47700 will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only taking a certain amount of U-47700.

Legality

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This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

  • Brazil - Possession, production and sale is illegal as it is listed on Portaria SVS/MS nº 344.[24]
  • Sweden - Following its sale as a designer drug, U-47700 was made illegal in Sweden on 26 January 2016.[25]
  • Finland - U-47700 is an Annex 1 drug in Finland, making its sale, production, and importation illegal.[26]
  • United Kingdom - U-447700 is a class A drug in the UK as of 31st May 2017 and is illegal to possess, produce or supply. [27]
  • United States - While U-47700 is not scheduled on a federal level, the State of Ohio recently made U-47700 a Schedule I drug. This is not a federal or nationwide action and can only be enforced in the state of Ohio.[28] On September 7th, 2016, the DEA Office of Diversion Control announced that they intend to schedule U-47700 as a Schedule temporarily I drug.[29]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. U-47700 at DistilBio | http://www.distilbio.com/show/compound/U-47700
  3. Jacob Szmuszkovicz (4 July 1978). "Patent US4098904 - Analgesic n-(2-aminocycloaliphatic)benzamides" | http://www.google.com/patents/US4098904
  4. Darrell D Mullins (28 June 1966). "Patent US US3258489 - N-(1-aminocyclohexylmethyl)anilines and n-(1-nitrocyclohexylmethyl)an-ilines". | http://www.google.com/patents/US3258489
  5. Norman James Harper, George Bryan Austin Veitch (17 August 1976). "Patent US3975443 - 1-(3,4-dichlorobenzamidomethyl)-cyclohexyldimethylamine". | http://www.google.com/patents/US3975443
  6. http://www.google.com/patents/US3510492
  7. Jacob Szmuszkovicz (5 May 1970). "Patent US3510492 - 2-anilino and 2-anilinomethyl cycloalkylamines". | http://www.google.com/patents/US3510492
  8. Ronald H Rynbrandt, Louis L Skaletzky (7 March 1972). "Patent US3647804 - Cycloalkanecarboxamides". | http://www.google.com/patents/US3510492
  9. W. Roll (23 July 1974). "Patent US3825595 - N-cyclopentyl-n-2-hydroxyalkyl-ring-substituted benzamides". | http://www.google.com/patents/US3825595
  10. Norman James Harper, George Bryan Austin Veitch (20 September 1977). "Patent US4049663 - Ethylene diamine derivatives".
  11. Alan F. Casy, Robert T. Parfitt (1986). Opioid Analgesics, Chemistry and Receptors. Springer US. p. 395. ISBN 978-1-4899-0587-1 | http://www.google.com/patents/US4049663
  12. Alan F. Casy, Robert T. Parfitt (1986). Opioid Analgesics, Chemistry and Receptors. Springer US. p. 395. ISBN 978-1-4899-0587-1. | http://link.springer.com/book/10.1007%2F978-1-4899-0585-7
  13. Medicinal agents incorporating the 1,2-diamine functionality. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2687936
  14. B. Vernon Cheney, Jacob Szmuszkovicz, Robert A. Lahti, Dominic A. Zichi (December 1985). "Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor". Journal of Medicinal Chemistry 28 (12): 1853–1864 | http://pubs.acs.org/doi/abs/10.1021/jm00150a017
  15. http://pubs.acs.org/doi/abs/10.1021/jm00257a012
  16. G. Loew, J. Lawson, L. Toll, G. Frenking, IP. Berzetei-Gurske, W. Polgar (1988). "Structure-activity studies of two classes of beta-amino-amides: the search for kappa-selective opioids." (PDF). NIDA Research Monograph 90: 144–151. | http://archives.drugabuse.gov/pdf/monographs/90.pdf
  17. Phenanthridone Analogs of the Opiate Agonist U-47,700 in the trans-1,2-Diaminocyclohexane Benzamide Series | http://www.heterocycles.jp/newlibrary/libraries/abst/07731
  18. U-50,488 moreover, the к receptor: A personalized account covering the period 1973 to 1990 | http://link.springer.com/chapter/10.1007%2F978-3-0348-8730-4_4
  19. http://www.bluelight.org/vb/threads/739960-Novel-opioid-U-47700-Mega-Thread-and-FAQ
  20. Twee doden in België door overdosis met fentanylpleisters | http://deredactie.be/cm/vrtnieuws/binnenland/1.2558454
  21. Synthetic opiate makers stay step ahead of US drug laws as overdose cases rise (the Guardian) | http://www.theguardian.com/world/2016/apr/11/synthetic-opiates-drug-laws-w-18-fentanyl
  22. Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2
  23. Siegel, S., Hinson, R., Krank, M., & McCully, J. (1982). Heroin “overdose” death: contribution of drug-associated environmental cues. Science, 216(4544), 436–437. https://doi.org/10.1126/science.7200260
  24. http://portal.anvisa.gov.br/documents/33868/3233596/55+-+RDC+N%C2%BA+143-2017-DOU.pdf/de80dc69-acb4-48b3-a6ac-1198993b0c1e
  25. https://www.folkhalsomyndigheten.se/nyheter-och-press/nyhetsarkiv/2015/november/31-nya-amnen-kan-klassas-som-narkotika-eller-halsofarlig-vara/
  26. Lääkeaineluettelo http://www.finlex.fi/fi/laki/kokoelma/2013/sk20130220.pdf
  27. The Misuse of Drugs Act 1971 (Amendment) Order 2017 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2017/634/made
  28. Executive Order 2016-01K | http://governor.ohio.gov/Portals/0/pdf/executiveOrders/Executive%20Order%202016-01K.pdf
  29. Schedules of Controlled Substances: Temporary Placement of U-47700 Into Schedule I |http://www.deadiversion.usdoj.gov/fed_regs/rules/2016/fr0907.htm