Nortilidine
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| Identifiers | |
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| CAS Number | 38677-94-0 |
| PubChem (CID) | 162321 |
| ChemSpider | 142535 |
| UNII | 7145G6817J |
| ChEBI |
CHEBI:77839  Y |
| ChEMBL | CHEMBL1614654 |
| Chemical and physical data | |
| Formula | C16H21NO2 |
| Molar mass | 259.3434 g/mol |
| 3D model (Jmol) | Interactive image |
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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 tilidine is also known[5] which has almost identical properties to nortilidine.[6]
See also
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.
- ↑ 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: Peptide receptor modulators | |
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