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U-47700: A Synthetic Opioid with Unique Characteristics
U-47700, a synthetic opioid belonging to the benzamide chemical class, elicits analgesic, sedating, relaxing, and euphoric effects upon administration.
Originally developed by Upjohn in the 1970s, U-47700 emerged as the most active compound from a series of related compounds, identified by exploring key functional groups. Upjohn secured numerous patents for these compounds.
Toxicity and Usage
The toxicity of U-47700 remains poorly understood, with limited historical human usage. It is currently available as a gray-area research chemical via online vendors. Reports indicate peculiar physical properties, including high causticity, which can pose risks, especially when injected. Using harm reduction practices is strongly advised when considering its use.
U-47700, an atypical benzamide-class opioid, comprises a core phenyl ring with chlorine atoms at carbons R3 and R4. An amine group links to this ring through a carbonyl group (C=O). The terminal nitrogen atom of the amide group connects to a methyl carbon and a substituted cyclohexane ring, with further substitution at R2 involving a dimethylamino group, forming U-47700's distinctive structure.
U-47700 selectively targets the µ-opioid receptor, boasting potency up to 7.5 times greater than morphine.
Mechanism of Action
Opioids achieve their effects by binding to and activating the μ-opioid receptor. This occurs because opioids structurally mimic endogenous endorphins naturally found in the body, working with the μ-opioid receptor set. This structural mimicry results in euphoria, pain relief, and anxiolytic effects, as endorphins reduce pain, induce sleepiness, and trigger pleasure. Their release can be triggered by pain, strenuous exercise, orgasm, or excitement.
Additional Receptor Activity
U-47700 may also act as an agonist for the kappa-opioid receptor system. Consequently, it serves as the basis for selective kappa-opioid receptor ligands like U-50488 and U-69,593, which share similar structures. Its structure has prompted further experimentation among chemists to assess whether rigid analogs maintain activity. While not used in medical practice, selective kappa ligands are utilized in research.
Euphoria and Relaxation: U-47700 induces a general sense of euphoria, relaxation, anxiety relief, and pain reduction, resembling oxycodone's effects.
Physical Euphoria: Users describe moderate physical comfort, warmth, and euphoria, though less intense than morphine or heroin.
Itchiness: Commonly triggers itchiness due to histamine reactions.
Respiratory Depression: At higher doses, respiratory depression may be more pronounced than with other opioids, potentially leading to severe breathing difficulties, unconsciousness, or even coma.
Sedation: At high doses, U-47700 produces more pronounced sedation than oxycodone.
Constipation, Cough Suppression, and Other Effects: U-47700 also leads to constipation, cough suppression, difficulty urinating, pupil constriction, decreased libido, and appetite suppression.
Cognitive Euphoria: While less intense than morphine or heroin, U-47700 can induce powerful feelings of emotional bliss, contentment, and happiness.
Anxiety Suppression: It helps alleviate anxiety.
Compulsive Redosing: Due to its short duration and addictive nature, users risk compulsive redosing, which can harm mucous membranes.
Dream Potentiation: U-47700 may enhance dreams.
After the drug's effects wear off, users often experience a "comedown" or "crash" characterized by:
Cognitive Fatigue: Mental tiredness.
Thought Deceleration: Slower thinking.
Anxiety and Depression: Feelings of anxiety and depression.
Irritability: Increased irritability.
Toxicity and Harm Potential
U-47700 has high toxicity relative to its dosage. Long-term use may lead to diminished libido, apathy, and memory loss. Mixing it with depressants like alcohol or benzodiazepines can be lethal.
The drug's crystals are corrosive to mucous membranes, potentially causing harm. Routine maintenance like rinsing the nasal cavity with water is crucial for insufflation users.
Warning: Vaporizing the substance can harm the lungs, and sublingual administration may damage oral tissues.
Combining U-47700 with fentanyl resulted in one fatality in Belgium. In the USA, at least 17 opioid overdoses and several deaths have been linked to U-47700 use.
Austria: Illegal to possess, produce, and sell.
Brazil: Illegal to possess, produce, and sell.
Finland: Illegal to sell, produce, and import.
Germany: Illegal to manufacture, import, possess, sell, or transfer without a license.
Russia: Classified as a Schedule I controlled substance.
Sweden: Made illegal following sale as a designer drug.
Switzerland: Controlled substance, named under Verzeichnis D.
United Kingdom: Classified as a Class A drug, illegal to possess, produce, or supply.
United States: In Ohio, it is a Schedule I drug; the DEA intended to temporarily schedule it at the federal level.
Czech Republic: Classified as a Schedule I controlled substance.