R-4066

From Wikipedia, the free encyclopedia

R-4066
Systematic (IUPAC) name
N-(3,3-diphenyl-4-oxohex-1-yl)-7,8-benzo-3-azaspiro[5.5]undecane
Identifiers
CAS number	101564-56-1
ATC code	?
PubChem	380029
Chemical data
Formula	C32H37NO
Mol. mass	451.641
SMILES	eMolecules & PubChem
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a drug which is an analogue of the opioid analgesic methadone, where the metabolically labile dimethylamino group has been replaced by a piperidinospiro group.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.

[edit] References

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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