Nortilidine: Difference between revisions
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'''Nortilidine'''<ref>US Patent 3792080 - Process for Substituted Cyclohexenes & it's Products</ref> is the [[active metabolite]] of the drug [[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<ref>J Clin Pharmacol. 2002 Nov ;42 (11):1257-61 - Sequential first-pass metabolism of nortilidine: the active metabolite of the synthetic opioid drug tilidine</ref> but virtually all of the opioid activity resides in the (1R,2S) isomer<ref>Opiates: George R. Lenz page 439</ref>. The (1S,2R) isomer has [[NMDA antagonist]] activity. The drug also acts as a [[dopamine reuptake inhibitor]]. |
'''Nortilidine'''<ref>US Patent 3792080 - Process for Substituted Cyclohexenes & it's Products</ref> is the [[active metabolite]] of the drug [[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<ref>J Clin Pharmacol. 2002 Nov ;42 (11):1257-61 - Sequential first-pass metabolism of nortilidine: the active metabolite of the synthetic opioid drug tilidine</ref> but virtually all of the opioid activity resides in the (1R,2S) isomer<ref>Opiates: George R. Lenz page 439, Table 9-30 (78)</ref>. The (1S,2R) isomer has [[NMDA antagonist]] activity. The drug also acts as a [[dopamine reuptake inhibitor]]. |
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==See also== |
==See also== |
Revision as of 16:32, 7 October 2012
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Chemical and physical data | |
Formula | H21NO2 |
Molar mass | 259.3434 g/mol g·mol−1 |
3D model (JSmol) | |
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Nortilidine[1] is the active metabolite of the drug 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 (1R,2S) isomer[3]. The (1S,2R) isomer has NMDA antagonist activity. The drug also acts as a dopamine reuptake inhibitor.