Nortilidine
Nortilidine[1] is the major active metabolite of tilidine. It is formed from tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine[2] but virtually all of the opioid activity resides in the (1S,2R) isomer.[3] The (1R,2S) isomer has NMDA antagonist activity. The drug also acts as a dopamine reuptake inhibitor.[4] The reversed-ester of nortilidine is also known[5] which has almost identical properties to nortilidine.[6]
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Formula | C16H21NO2 |
Molar mass | 259.349 g·mol−1 |
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See also
- O-Desmethyltramadol, another opioid metabolite with additional (non-opioid) mechanisms of analgesia
References
- US Patent 3792080 - Process for Substituted Cyclohexenes its Products
- J Clin Pharmacol. 2002 Nov ;42 (11):1257-61 - Sequential first-pass metabolism of nortilidine: the active metabolite of the synthetic opioid drug tilidine
- Opiates: George R. Lenz page 439, Table 9-30 (78)
- Schifano, Fabrizio; Orsolini, Laura; Duccio Papanti, G.; Corkery, John M. (2015). "Novel psychoactive substances of interest for psychiatry". World Psychiatry. 14 (1): 15–26. doi:10.1002/wps.20174. ISSN 1723-8617. PMC 4329884. PMID 25655145.
- US Patent 4291059 - Cycloaromatic compounds, analgesic Properties thereof and Method of use thereof as analgesic
- Personal Communication with Derek P. Reynolds
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See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators |
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