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Norketamine
Norketamine, or ''N''-desmethylketamine, is the major active metabolite of ketamine, which is formed mainly by CYP3A4. Similarly to ketamine, norketamine acts as a noncompetitive NMDA receptor antagonist (Ki = 1.7 µM and 13 µM for (''S'')-(+)-norketamine and (''R'')-(–)-norketamine, respectively),〔 but is about 3–5 times less potent as an anesthetic in comparison.〔 Also, similarly again to ketamine, norketamine binds to the μ- and κ-opioid receptors. Relative to ketamine, norketamine is much more potent as an antagonist of the α7-nicotinic acetylcholine receptor, and produces rapid antidepressant effects in animal models which have been reported to correlate with its activity at this receptor. However, norketamine is about 1/5th as potent as ketamine as an antidepressant in mice as per the forced swim test, and this seems also to be in accordance with its 3–5-fold reduced comparative potency ''in vivo'' as an NMDA receptor antagonist. Norketamine is metabolized into dehydronorketamine, which is far less active as an NMDA receptor antagonist in comparison〔 but retains activity as a potent antagonist of the α7-nicotinic acetylcholine receptor.
==See also==
* Arketamine
* Esketamine
* Hydroxynorketamine
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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