KNT-63(KNT-63) - 药物靶点：κ opioid receptor_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

作用方式

激动剂

作用机制

κ opioid receptor激动剂(κ-阿片受体激动剂)

治疗领域

神经系统疾病其他疾病

在研适应症-

非在研适应症

疼痛

原研机构

Kitasato University

在研机构-

非在研机构

Kitasato University

权益机构-

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 KNT-63 相关的临床结果

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100 项与 KNT-63 相关的转化医学

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100 项与 KNT-63 相关的专利（医药）

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2

项与 KNT-63 相关的文献（医药）

2014-11-01·Bioorganic & medicinal chemistry letters4区 · 医学

Design, synthesis, and structure–activity relationship of novel opioid κ receptor selective agonists: α-Iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton

4区 · 医学

Article

作者: Gouda, Hiroaki ; Watanabe, Yoshikazu ; Nagasea, Hiroshi ; Hirayama, Shigeto ; Kitazawa, Shota ; Hirono, Shuichi ; Iwai, Takashi ; Fujii, Hideaki ; Nemoto, Toru

The α-iminoamide derivative, 4b was designed and synthesized as a novel agonist selective for the opioid κ receptor. The amide was constrained to an orientation horizontal to the F-ring of the azabicyclo[2.2.2]octane skeleton, which remarkably improved its affinity, selectivity, and agonistic activity for the κ receptor. This finding was newly established by chemical modification of the nitrogen atom at the 8-position in the azabicyclo[2.2.2]octane skeleton. This modification would never have been found with KNT-63, a derivation of oxabicyclo[2.2.2]octane. These results may provide valuable information for the future development of novel κ selective agonists.

2010-01-01·Bioorganic & medicinal chemistry letters4区 · 医学

Drug design and synthesis of a novel κ opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology

4区 · 医学

Article

作者: Hayashida, Kohei ; Nakao, Kaoru ; Hasebe, Ko ; Nagase, Hiroshi ; Hirono, Shuichi ; Yamaotsu, Noriyuki ; Nemoto, Toru ; Fujii, Hideaki ; Nakajima, Mayumi ; Mochizuki, Hidenori ; Watanabe, Akio

A conformational analysis of kappa opioid receptor agonists, TRK-820 and U-50,488H indicated an active conformation of TRK-820 in which the C-ring was in the boat form with the 14-OH interacting with the amide nitrogen. Based on the obtained active conformation of TRK-820, we designed and synthesized a novel kappa agonist KNT-63 with oxabicyclo[2.2.2]octane skeleton. KNT-63 showed profound antinociceptive effects via the kappa receptor which were as potent as that of TRK-820.

100 项与 KNT-63 相关的药物交易

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