
U-47700: Difference between revisions
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*'''[[Effect::Anxiety suppression]]''' | *'''[[Effect::Anxiety suppression]]''' | ||
*'''[[Effect::Compulsive redosing]]''' | *'''[[Effect::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: | |||
*'''[[Effect::Cognitive fatigue]]''' | |||
*'''[[Effect::Thought deceleration]]''' | |||
*'''[[Effect::Anxiety]]''' | |||
*'''[[Effect::Depression]]''' | |||
*'''[[Effect::Irritability]]''' | |||
==Toxicity and harm potential== | ==Toxicity and harm potential== |
Revision as of 21:14, 26 April 2016
U-47700 | |||||||||||||||||||||||||||||||
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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 | ||||||||||||||||||||||||||||||
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Summary sheet: U-47700 |
U-47700[1] is a opioid within the benzamide chemical class which was developed by a team at Upjohn in the 1970s[2] and is available today through the use of online research chemical vendors.
U-47700 is the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold. The team looked for the key moieties which gave the greatest activity.[5] Upjohn posted over a dozen patents on related compounds, each optimizing one moiety[6][7][8][9][10][11][12] until they discovered that U-47700 was the most active.[13]
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.[3][4] 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 became the lead compound of selective kappa-opioid receptor ligands such as U-50488 (containing a single methylene spacer difference) and U-69,593, which share very similar structures.[14] Its structure led to other chemists experimenting with it to see if rigid analogues would retain activity.[15] Although not used medically, the selective kappa ligands are used in research.[16]
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 - 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
U-47700 has a high toxicity relative to its dose due to its extreme potency. As with all opiates, 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]].
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 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. |
See also
External links
References
- ↑ U-47700 at DistilBio | http://www.distilbio.com/show/compound/U-47700