苯环己定
化学
NMDA受体
亲脂性
立体化学
氯胺酮
内酰胺
药理学
受体
致幻剂
效力
体外
生物化学
神经科学
医学
生物
作者
Paola Zarantonello,Ezio Bettini,Alfredo Paio,Chiara Simoncelli,Silvia Terreni,Francesco Cardullo
标识
DOI:10.1016/j.bmcl.2011.02.009
摘要
The identification of structurally novel analogues of ketamine and phencyclidine (PCP), as NMDA receptor antagonists, with low to moderate potency at GluN2A and GluN2B receptors is discussed. In particular, some examples, such as compounds 6 and 10, shows decreased calculated lipophilicity, when compared to PCP, while retaining moderate activity. Moreover, the germinal aryl amino substituted lactam ring, as exemplified in compounds 7–10 and 11–13, constitutes a novel scaffold with potential application in the design of biologically active compounds.
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