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| {{SubstanceBox/U-47700}}
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| | ''[[U-47700/Summary|Summary sheet: U-47700]]''
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| '''U-47700'''<ref>U-47700 at DistilBio | http://www.distilbio.com/show/compound/U-47700</ref> is an [[psychoactive class::opioid]] within the [[chemical class::benzamide]] chemical class. It has very little history of human usage and is currently available through the use of certain online [[research chemical]] vendors.
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| This compound was initially developed by a team at Upjohn in the 1970s.<ref> Jacob Szmuszkovicz (4 July 1978). "Patent US4098904 - Analgesic n-(2-aminocycloaliphatic)benzamides" | http://www.google.com/patents/US4098904</ref> Upjohn created over a dozen patents on related compounds<ref>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</ref><ref>Norman James Harper, George Bryan Austin Veitch (17 August 1976). "Patent US3975443 - 1-(3,4-dichlorobenzamidomethyl)-cyclohexyldimethylamine". | http://www.google.com/patents/US3975443</ref><ref>http://www.google.com/patents/US3510492</ref><ref>Jacob Szmuszkovicz (5 May 1970). "Patent US3510492 - 2-anilino and 2-anilinomethyl cycloalkylamines". | http://www.google.com/patents/US3510492</ref><ref> Ronald H Rynbrandt, Louis L Skaletzky (7 March 1972). "Patent US3647804 - Cycloalkanecarboxamides". | http://www.google.com/patents/US3510492</ref><ref>W. Roll (23 July 1974). "Patent US3825595 - N-cyclopentyl-n-2-hydroxyalkyl-ring-substituted benzamides". | http://www.google.com/patents/US3825595</ref><ref>Norman James Harper, George Bryan Austin Veitch (20 September 1977). "Patent US4049663 - Ethylene diamine derivatives".</ref><ref> 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</ref> until they discovered that U-47700 was the most active.<ref>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</ref> This was done by looking for the key functional groups which gave the greatest activity.<ref>Medicinal agents incorporating the 1,2-diamine functionality. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2687936</ref>
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| ==Chemistry==
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| {{chemistry}}
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| ==Pharmacology==
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| U-47700 is selective for the µ-opioid receptor, having around 7.5x the potency of morphine in animal models.<ref>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</ref><ref>http://pubs.acs.org/doi/abs/10.1021/jm00257a012</ref>
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| Opioids exert their effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|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 [[physical euphoria|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.
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| 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.<ref>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</ref> Its structure led to other chemists experimenting with it to see if rigid analogues would retain activity.<ref>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</ref> Although not used medically, the selective kappa ligands are used in research.<ref>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</ref>
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| ==Subjective effects==
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| The effects listed below are based upon the [[subjective effects index]] and personal experiences of [[PsychonautWiki]] [[Special:TopUsers|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.
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| ===Physical effects===
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| The general head space of U-47700 is described by many as one of euphoria, relaxation, anxiety suppression and pain relief.
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| *'''[[Effect::Pain relief]]'''
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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.
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| *'''[[Effect::Itchiness]]''' - This compound presents greater amounts of itchiness due to higher amounts of histamine release in comparison to other [[opioids]].
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| *'''[[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.
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| *'''[[Effect::Sedation]]''' - At higher dosages, this compound can result in feelings of sedation and is considerably more sedating than that of [[oxycodone]] and [[hydrocodone]].
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| *'''[[Effect::Constipation]]'''
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| *'''[[Effect::Cough suppression]]'''
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| *'''[[Effect::Difficulty urinating]]'''
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| *'''[[Effect::Pupil constriction]]'''
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| ===Cognitive effects===
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| *'''[[Effect::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.
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| *'''[[Effect::Anxiety suppression]]'''
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| *'''[[Effect::Compulsive redosing]]'''
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| ===After effects===
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| 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" or "crash". Its effects commonly include:
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| *'''[[Effect::Cognitive fatigue]]'''
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| *'''[[Effect::Thought deceleration]]'''
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| *'''[[Effect::Anxiety]]'''
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| *'''[[Effect::Depression]]'''
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| *'''[[Effect::Irritability]]'''
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| ==Toxicity and harm potential==
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| {{Main|Research chemicals#Toxicity and harm potential}}
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| U-47700 has a [[Toxicity::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 [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[benzodiazepines]]]].
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| 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.
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| Combined consumption of U-47700 and [[fentanyl]] caused one fatality in Belgium.<ref>Twee doden in België door overdosis met fentanylpleisters | http://deredactie.be/cm/vrtnieuws/binnenland/1.2558454</ref> At least 17 opioid overdoses and several deaths in the USA have also been connected with the use of U-47700.<ref>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</ref>
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| It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug.
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| ===Tolerance and addiction potential===
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| As with other [[opioids]], the chronic use of U-47700 can be considered [[Addiction potential::moderately addictive with a high potential for abuse]] and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and [[Opioids#Discontinuation|withdrawal symptoms]] may occur if a person suddenly stops their usage.
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| Tolerance to many of the effects of U-47700 [[Time to full tolerance::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 [[Time to half tolerance::3 - 7 days]] for the tolerance to be reduced to half and [[Time to zero tolerance::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 [[opioid]]s will have a reduced effect.
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| ===Dangerous interactions===
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| 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. [https://www.google.com/ Independent research] should always be done to ensure that a combination of two or more substances is safe before consumption.
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| *'''[[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 [https://www.youtube.com/watch?v=uCDa-AhrjHo recovery position] or have a friend move them into it.
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| *'''[[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 [https://www.youtube.com/watch?v=uCDa-AhrjHo recovery position] or have a friend move them into it.
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| *'''[[Stimulants]]''' - It is dangerous to combine U-47700, a [[depressant]], with [[stimulant]]s due to the risk of excessive intoxication. Stimulants decrease the [[sedation|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 [[U-47700#Subjective effects|other effects]]. If combined, one should strictly limit themselves to only taking a certain amount of U-47700.
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| ==Legal issues==
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| {{legalStub}}
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| *'''Sweden''' - Following its sale as a [[designer drug]], U-47700 was made illegal in Sweden on 26 January 2016.<ref>https://www.folkhalsomyndigheten.se/nyheter-och-press/nyhetsarkiv/2015/november/31-nya-amnen-kan-klassas-som-narkotika-eller-halsofarlig-vara/</ref>
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| *'''United Kingdom''' - This drug is illegal under the Psychoactive Substance Act, which came into effect on May 26th, 2016.<ref>Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted</ref>
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| ==See also==
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| *[[Responsible use]]
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| *[[Depressants]]
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| *[[Opioid]]
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| ==External links==
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| *[https://en.wikipedia.org/wiki/U-47700 U-47700 (Wikipedia)]
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| *[http://www.bluelight.org/vb/threads/739960-Novel-opioid-U-47700 U-47700 (Bluelight)]
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| *[https://www.reddit.com/r/researchchemicals/comments/35y8b4/been_experimenting_with_u47700_the_last_few_days/ U-44770 (Reddit)]
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| =References=
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| <references />
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| [[Category:Psychoactive substance]]
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| [[Category:Morphinan]]
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| [[Category:Depressant]]
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| {{#set:Featured=true}}
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