NP-5497-KA(NP-5497-KA) - 药物靶点：κ opioid receptor_在研适应症：阿片类药物过量_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

κ opioid receptor

作用机制

κ opioid receptor激动剂(κ-阿片受体激动剂)

治疗领域

其他疾病

在研适应症

阿片类药物过量

非在研适应症-

原研机构

Tokyo Metropolitan Institute of Medical Science

Nippon Chemiphar Co., Ltd.

在研机构

Tokyo Metropolitan Institute of Medical Science

Nippon Chemiphar Co., Ltd.

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 NP-5497-KA 相关的临床结果

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100 项与 NP-5497-KA 相关的转化医学

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100 项与 NP-5497-KA 相关的专利（医药）

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1

项与 NP-5497-KA 相关的文献（医药）

Scientific Reports

Effects of the novel selective κ-opioid receptor agonist NP-5497-KA on morphine-induced reward-related behaviors

Article

作者: Yamakawa, Tomio ; Ide, Soichiro ; Ikeda, Kazutaka ; Muto, Takafumi ; Hirai, Toshitake

AbstractOpioid addiction and the opioid overdose epidemic are becoming more serious, and the development of therapeutic agents is essential for the pharmacological treatment of substance use disorders. The κ-opioid receptor (KOP) is a member of the opioid receptor system that has been gaining attention as a promising molecular target for the treatment of numerous human disorders, including pain, depression, anxiety, and drug addiction. Here, we biologically and pharmacologically evaluated a novel azepane-derived ligand, NP-5497-KA, as a selective KOP agonist. NP-5497-KA had 1000-fold higher selectivity for the KOP over the μ-opioid receptor (MOP), which was higher than nalfurafine (KOP/MOP: 65-fold), and acted as a selective KOP full agonist in the 3′,5′-cyclic adenosine monophosphate assay. The oral administration of NP-5497-KA (1–10 mg/kg) dose-dependently suppressed morphine-induced conditioned place preference in C57BL/6 J mice, and its effects were comparable to an intraperitoneal injection of nalfurafine (1–10 μg/kg). Nalfurafine (10 μg/kg) significantly inhibited rotarod performance, whereas NP-5497-KA (10 mg/kg) exerted no effect on rotarod performance. These results indicate that NP-5497-KA may be a novel option for the treatment of opioid use disorder with fewer side effects.

100 项与 NP-5497-KA 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
阿片类药物过量	临床前	日本	Nippon Chemiphar Co., Ltd.	2023-10-24
阿片类药物过量	临床前	日本	Tokyo Metropolitan Institute of Medical Science	2023-10-24