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(Rac)-Lanicemine((Rac)-AZD6765)是Lanicemine的外消旋体。Lanicemine(AZD6765)是一种低捕获的NMDA受体拮抗剂,Ki为0.56-2.1 μM。CHO和爪蟾卵母细胞中,IC50分别为4-7μM和6.4μM。具有抗抑郁作用。
(Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects[1].
Lanicemine produces sustained antidepressant efficacy with minimal psychotomimetic adverse effects[1].Lanicemine (3, 10 or 30 mg/kg; intraperitoneal) not only engages brain circuits involved in the generation of gamma- electroencephalography (EEG), but also influences these networks independent of the broader systems-level disruptions typical of ketamine[1]. Animal Model: Male Sprague-Dawley rats[1]
[1]. Sanacora G, et al. Lanicemine: a low-trapping NMDA channel blocker produces sustained antidepressant efficacywith minimal psychotomimetic adverse effects. Mol Psychiatry. 2014 Sep;19(9):978-85.
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