Chemistry:R-4066
From HandWiki
R-4066 (Spirodone) is a drug which is a derivative of the opioid analgesic norpipanone, wherein the piperidine ring has been replaced by a tricyclic spiro heterocycle. Developed by Janssen Pharmaceutica,[1] it is around 212× more potent than methadone as an analgesic in animal tests, with an effective oral dosage of 0.07 mg/kg, but is shorter acting, with a duration of action of around 3 hours. If the ketone function is reduced and acetylated, the racemate has a potency of 106× that of methadone and has an analgesic duration of 20.5 hours compared to 8 hours for methadone.[2]
Other related compounds include R-4837 [59708-47-3] & R-5260 [1109-69-9].[3]
References
- ↑ U.S. Patent 3,125,580
- ↑ "Synthesis and analgesic activity of some long-acting piperidinospiro derivatives of methadone". Journal of Medicinal Chemistry 21 (5): 474–6. May 1978. doi:10.1021/jm00203a014. PMID 660594.
- ↑ "Differentiation of opiate and neuroleptic receptor binding in rat brain". European Journal of Pharmacology 43 (3): 253–267. June 1977. doi:10.1016/0014-2999(77)90025-5.
 | 0.00  (0 votes) |
