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U-47700: Difference between revisions
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U-47700 is selective for the µ-opioid receptor, with various sources claiming 7.5x the potency of morphine.<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> | U-47700 is selective for the µ-opioid receptor, with various sources claiming 7.5x the potency of morphine.<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> | ||
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 | 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 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 [[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. | ||
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 | 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 analogs 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 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</ref> | ||
==Subjective effects== | ==Subjective effects== | ||
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===Cognitive effects=== | ===Cognitive effects=== | ||
*'''[[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 its short duration and structural differences. 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. | *'''[[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 its short duration and structural differences. 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 a powerful and overwhelming feeling of emotional bliss, contentment, and happiness. | ||
*'''[[Effect::Anxiety suppression]]''' | *'''[[Effect::Anxiety suppression]]''' | ||
*'''[[Effect::Compulsive redosing]]''' - Due to the short duration of this substance | *'''[[Effect::Compulsive redosing]]''' - Due to the short duration of this substance and the addictive properties of opioids in general, there is a strong risk of compulsive redosing which is considerably dangerous considering it is very corrosive to mucous membranes. | ||
*'''[[Effect::Dream potentiation]]''' | *'''[[Effect::Dream potentiation]]''' | ||
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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]]]]. | 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]]]]. | ||
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 | 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.<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 | 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> | ||
It is strongly recommended that one use [[responsible drug use|harm reduction practices]], and take extreme caution when using this substance. | It is strongly recommended that one use [[responsible drug use|harm reduction practices]], and take extreme caution when using this substance. | ||
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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. | 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. | ||
[[U-47700]] withdrawal symptoms can be especially painful and emerge after 2-4 hours after the last dose administration. It is highly advisable to | [[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.<ref>Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2</ref> 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.<ref>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</ref> | The risk of fatal opioid overdoses rise sharply after a period of cessation and [[relapse]], largely because of reduced tolerance.<ref>Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2</ref> 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.<ref>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</ref> | ||
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{{legalStub}} | {{legalStub}} | ||
*'''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> | *'''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> | ||
*'''Finland''' - U-47700 is an Annex 1 drug in Finland, making its sale, production and importation illegal.<ref> Lääkeaineluettelo http://www.finlex.fi/fi/laki/kokoelma/2013/sk20130220.pdf</ref> | *'''Finland''' - U-47700 is an Annex 1 drug in Finland, making its sale, production, and importation illegal.<ref> Lääkeaineluettelo http://www.finlex.fi/fi/laki/kokoelma/2013/sk20130220.pdf</ref> | ||
*'''United Kingdom''' - It is illegal to produce, supply, or import this drug 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> | *'''United Kingdom''' - It is illegal to produce, supply, or import this drug 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> | ||
*'''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.<ref>Executive Order 2016-01K | http://governor.ohio.gov/Portals/0/pdf/executiveOrders/Executive%20Order%202016-01K.pdf</ref> On September 7th, 2016, the DEA Office of Diversion Control announced that they intend to | *'''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.<ref>Executive Order 2016-01K | http://governor.ohio.gov/Portals/0/pdf/executiveOrders/Executive%20Order%202016-01K.pdf</ref> On September 7th, 2016, the DEA Office of Diversion Control announced that they intend to schedule U-47700 as a Schedule temporarily I drug.<ref>Schedules of Controlled Substances: Temporary Placement of U-47700 Into Schedule I |http://www.deadiversion.usdoj.gov/fed_regs/rules/2016/fr0907.htm</ref> | ||
==See also== | ==See also== | ||