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Hydroxynorketamine
Hydroxynorketamine (HNK), or 6-hydroxynorketamine, is a metabolite of ketamine which is formed by hydroxylation of its metabolite norketamine. In contrast to ketamine and norketamine, hydroxynorketamine is inactive as an anesthetic and psychostimulant. In accordance, it has only very weak affinity for the NMDA receptor (Ki = 21.19 µM and > 100 μM for (2''S'',6''S'')-hydroxynorketamine and (2''R'',6''R'')-hydroxynorketamine, respectively). However, hydroxynorketamine does still show biological activity, having been found to act as a potent and selective negative allosteric modulator of the α7-nicotinic acetylcholine receptor (IC50 < 1 µM).〔 Moreover, (2''S'',6''S'')-hydroxynorketamine was tested and was found to increase the function of the mammalian target of rapamycin (mTOR), a marker of the antidepressant activity of ketamine, far more potently than ketamine itself (0.05 nM for (2''S'',6''S'')-hydroxynorketamine, 10 nM for (''S'')-norketamine, and 1,000 nM for (''S'')-ketamine (esketamine), respectively), an action that was observed to correlate closely with their ability to inhibit the α7-nicotinic acetylcholine receptor. This finding has led to a call of reassessment of the understanding of the rapid antidepressant effects of ketamine and their mechanisms. However, subsequent research has found that dehydronorketamine, which is a potent and select antagonist of the α7-nicotinic acetylcholine receptor similarly to hydroxynorketamine, is inactive in the forced swim test at doses up to 50 mg/kg in mice, and this is in contrast to ketamine and norketamine, which are effective at doses of 10 mg/kg and 50 mg/kg, respectively. This is likely due to the far lower potency of dehydronorketamine as an NMDA receptor antagonist in comparison.〔
==See also==
* Arketamine
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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