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*'''[[Effect::Physical euphoria]]''' - This particular substance can be considered as less intense in its physical euphoria when compared with that of [[morphine]] or [[diacetylmorphine]] (heroin) due to the upper limit of how much can be converted into its active form through metabolism. The sensation itself can be described as extreme feelings of intense physical comfort, warmth and physical blissful euphoria which spreads throughout the body.
*'''[[Effect::Physical euphoria]]''' - This particular substance can be considered as less intense in its physical euphoria when compared with that of [[morphine]] or [[diacetylmorphine]] (heroin) due to the upper limit of how much can be converted into its active form through metabolism. The sensation itself can be described as extreme feelings of intense physical comfort, warmth and physical blissful euphoria which spreads throughout the body.
*'''[[Effect::Itchiness]]''' - This compound presents greater amounts of itchiness due to higher amounts of histamine release in comparison to other [[opioids]].
*'''[[Effect::Itchiness]]''' - This compound presents greater amounts of itchiness due to higher amounts of histamine release in comparison to other [[opioids]].
*'''[[Effect::Respiratory depression]]''' - Although it has not been formally studied, annecdotal reports suggest that respiratory depression is significantly stronger with this compound in comparison to other more common opioids such as [[heroin and [[morphine]]. At low to moderate doses, this effect results in the sensation that the breath is slowed down mildly to moderately, but does not cause noticeable impairment. At high doses and overdoses, opioid-induced respiratory depression can result in a shortness of breath, abnormal breathing patterns, semi-consciousness, or unconsciousness. Severe overdoses can result in a coma or death without immediate medical attention.
*'''[[Effect::Respiratory depression]]''' - Although it has not been formally studied, annecdotal reports suggest that respiratory depression is significantly stronger with this compound in comparison to other more common opioids such as [[heroin]] and [[morphine]]. At low to moderate doses, this effect results in the sensation that the breath is slowed down mildly to moderately, but does not cause noticeable impairment. At high doses and overdoses, opioid-induced respiratory depression can result in a shortness of breath, abnormal breathing patterns, semi-consciousness, or unconsciousness. Severe overdoses can result in a coma or death without immediate medical attention.
*'''[[Effect::Sedation]]''' - At higher dosages, this compound can result in feelings of sedation and is considerably more sedating than that of [[oxycodone]] and [[hydrocodone]].
*'''[[Effect::Sedation]]''' - At higher dosages, this compound can result in feelings of sedation and is considerably more sedating than that of [[oxycodone]] and [[hydrocodone]].
*'''[[Effect::Constipation]]'''
*'''[[Effect::Constipation]]'''

Revision as of 21:43, 21 May 2016

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U-47700
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 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.

Interactions
Stimulants
MAOIs
Nitrous
PCP
Alcohol
Benzodiazepines
DXM
GHB
GBL
Ketamine
MXE
Tramadol
Grapefruit
Summary sheet: U-47700

U-47700[1] is a opioid within the benzamide chemical class. It has very little history of human usage and is currently available through the use of certain online research chemical vendors.

This compound was initially developed by a team at Upjohn in the 1970s.[2] Upjohn created over a dozen patents on related compounds[3][4][5][6][7][8][9][10] until they discovered that U-47700 was the most active.[11] This was done by looking for the key functional groups which gave the greatest activity.[12]

Chemistry

This chemistry section is incomplete.

You can help by adding to it.

Pharmacology

U-47700 is selective for the µ-opioid receptor, having around 7.5 x the potency of morphine in animal models.[13][14]

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 within the body and also work upon 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. In day to day life, they can be released in response to pain, strenuous exercise, orgasm, or general excitement.

U-47700 is also 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.[15] Its structure led to other chemists experimenting with it to see if rigid analogues would retain activity.[16] Although not used medically, the selective kappa ligands are used in research.[17]

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

The general head space of U-47700 is described by many as one of euphoria, relaxation, anxiety suppression and pain relief.

  • Pain relief
  • Physical euphoria - This particular substance can be considered as less intense in its physical euphoria when compared with that of morphine or diacetylmorphine (heroin) due to the upper limit of how much can be converted into its active form through metabolism. The sensation itself can be described as extreme feelings of intense physical comfort, warmth and physical blissful euphoria which spreads throughout the body.
  • Itchiness - This compound presents greater amounts of itchiness due to higher amounts of histamine release in comparison to other opioids.
  • Respiratory depression - Although it has not been formally studied, annecdotal reports suggest that respiratory depression is significantly stronger with this compound in comparison to other more common opioids such as heroin and morphine. At low to moderate doses, this effect results in the sensation that the breath is slowed down mildly to moderately, but does not cause noticeable impairment. At high doses and overdoses, opioid-induced respiratory depression can result in a shortness of breath, abnormal breathing patterns, semi-consciousness, or unconsciousness. Severe overdoses can result in a coma or death without immediate medical attention.
  • Sedation - At higher dosages, this compound can result in feelings of sedation and is considerably more sedating than that of oxycodone and hydrocodone.
  • Constipation
  • Cough suppression
  • Difficulty urinating
  • Pupil constriction

Cognitive effects

  • Cognitive euphoria - This particular substance can be considered as less intense in its cognitive euphoria when compared with that of morphine or diacetylmorphine (heroin) due to the upper limit of how much can be converted into its active form through metabolism. It is still, however, capable of extreme intensity and overwhelming bliss at heavier dosages with a low tolerance. The sensation itself can be described as powerful and overwhelming feeling of emotional bliss, contentment, and happiness.
  • Anxiety suppression
  • Compulsive redosing

After effects

Unlike most other opioids, the effects which occur during the offset of this compound generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and likely occurs because of U-47700's affinity to kappa receptors. Its effects commonly include:

Toxicity and harm potential

Main article: Research chemicals § 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 [[Toxicity::potentially lethal when mixed with depressants like alcohol or benzodiazepines]].

Combined consumption of U-47700 and fentanyl caused one fatality in Belgium.[18] At least 17 opioid overdoses and several deaths in the USA have also been connected with the use of U-47700.[19]

It is strongly recommended that one use harm reduction practices when using this drug.

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 [[Cross-tolerance::all other opioids]], meaning that after the consumption of U-47700 all opioids will have a reduced effect.

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 also 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 depressants, 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

This legality section is a stub.

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

  • Sweden - Following its sale as a designer drug, U-47700 was made illegal in Sweden on 26 January 2016.[20]

See also

References

  1. ↑ U-47700 at DistilBio | http://www.distilbio.com/show/compound/U-47700
  2. ↑ Jacob Szmuszkovicz (4 July 1978). "Patent US4098904 - Analgesic n-(2-aminocycloaliphatic)benzamides" | http://www.google.com/patents/US4098904
  3. ↑ 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
  4. ↑ Norman James Harper, George Bryan Austin Veitch (17 August 1976). "Patent US3975443 - 1-(3,4-dichlorobenzamidomethyl)-cyclohexyldimethylamine". | http://www.google.com/patents/US3975443
  5. ↑ http://www.google.com/patents/US3510492
  6. ↑ Jacob Szmuszkovicz (5 May 1970). "Patent US3510492 - 2-anilino and 2-anilinomethyl cycloalkylamines". | http://www.google.com/patents/US3510492
  7. ↑ Ronald H Rynbrandt, Louis L Skaletzky (7 March 1972). "Patent US3647804 - Cycloalkanecarboxamides". | http://www.google.com/patents/US3510492
  8. ↑ W. Roll (23 July 1974). "Patent US3825595 - N-cyclopentyl-n-2-hydroxyalkyl-ring-substituted benzamides". | http://www.google.com/patents/US3825595
  9. ↑ Norman James Harper, George Bryan Austin Veitch (20 September 1977). "Patent US4049663 - Ethylene diamine derivatives".
  10. ↑ 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
  11. ↑ 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
  12. ↑ Medicinal agents incorporating the 1,2-diamine functionality. | https://www.ncbi.nlm.nih.gov/pubmed/2687936
  13. ↑ 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
  14. ↑ http://pubs.acs.org/doi/abs/10.1021/jm00257a012
  15. ↑ 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
  16. ↑ 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
  17. ↑ U-50,488 and 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
  18. ↑ Twee doden in België door overdosis met fentanylpleisters | http://deredactie.be/cm/vrtnieuws/binnenland/1.2558454
  19. ↑ 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
  20. ↑ https://www.folkhalsomyndigheten.se/nyheter-och-press/nyhetsarkiv/2015/november/31-nya-amnen-kan-klassas-som-narkotika-eller-halsofarlig-vara/
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