δ 阿片受体完全反向激动剂的发现及其对束缚应激诱导的小鼠认知功能障碍的影响。
Discovery of δ Opioid Receptor Full Inverse Agonists and Their Effects on Restraint Stress-Induced Cognitive Impairment in Mice.
机构信息
Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
Medicinal Research Laboratories, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
出版信息
ACS Chem Neurosci. 2019 May 15;10(5):2237-2242. doi: 10.1021/acschemneuro.9b00067. Epub 2019 Apr 1.
The cyclopropylmethyl group in classical δ opioid receptor (DOR) antagonist NTI, BNTX, and NTB was replaced with various electron-withdrawing groups to develop DOR inverse agonists. N-Benzyl NTB derivative SYK-657 was a potent DOR full inverse agonist and its potency was over 10-fold potent than that of a reference compound ICI-174,864. Intraperitoneal administration of SYK-657 induced the short-term memory improving effect in mice without abnormal behaviors.
经典 δ 阿片受体（DOR）拮抗剂 NTI、BNTX 和 NTB 中的环丙甲基基团被各种吸电子基团取代，以开发 DOR 反向激动剂。N-苄基 NTB 衍生物 SYK-657 是一种有效的 DOR 完全反向激动剂，其效力超过参考化合物 ICI-174,864 的 10 倍以上。SYK-657 腹腔给药可诱导小鼠产生短期记忆改善作用，而无异常行为。
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