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R-4066: Wikis


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Systematic (IUPAC) name
CAS number 101564-56-1
ATC code  ?
PubChem 380029
Chemical data
Formula C 32H37NO 
Mol. mass 451.641
SMILES eMolecules & PubChem
Synonyms N-(3,3-diphenyl-4-oxohex-1-yl)-7,8-benzo-3-azaspiro[5.5]undecane
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

R-4066 is a drug which is an analogue of the opioid analgesic methadone, where the metabolically labile dimethylamino group has been replaced by a piperidinospiro group. It is around 212x more potent than methadone as an analgesic in animal tests, with an effective oral dosage of 0.07mg/kg, but is slightly shorter acting, with a duration of action of around 3 hours.[1]

R-4066 has never been used in humans, but would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching and respiratory depression which could be harmful or fatal.


  1. ^ Frincke JM, Henderson GL, Janssen PAJ, Van der Eycken CAM. Synthesis and analgesic activity of some long-acting piperidinospiro derivatives of methadone. Journal of Medicinal Chemistry. 1978 May;21(5):474-6. PMID 660594


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