AA-501(AA-501) - 药物靶点：NK1R_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

NK1R

作用机制

NK1调节剂(神经激肽-1-受体调节剂)

治疗领域

神经系统疾病

在研适应症-

非在研适应症

疼痛

原研机构

Tufts University School of Medicine

在研机构-

非在研机构

Tufts University School of Medicine

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 AA-501 相关的临床结果

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100 项与 AA-501 相关的转化医学

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100 项与 AA-501 相关的专利（医药）

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1

项与 AA-501 相关的文献（医药）

2004-03-01·European Journal of Pharmacology3区 · 医学

Spinal antinociceptive effects of AA501, a novel chimeric peptide with opioid receptor agonist and tachykinin receptor antagonist moieties

3区 · 医学

Article

作者: Andrzej W. Lipkowski ; Stacy E. Foran ; James E. Marchand ; Iwona Maszczynska Bonney ; Daniel B. Carr

The use of "multimodal" combination analgesic therapies or novel single molecules possessing multiple analgesic targets is becoming increasingly attractive. In previous experiments we showed that a substance P antagonist injected intrathecally potentiated the antinociceptive effects of potent opioid receptor agonist, biphalin. Based on examination of the biphalin structure-activity relationship, we designed and synthesized a novel chimeric peptide, termed AA501 (N'(Tyr-D-Ala-Gly-Phe), N"(Z-Trp) hydrazide, Z=benzyloxycarbonyl). AA501 consists of an opioid receptor agonist pharmacophore related to biphalin and a substance P receptor antagonist pharmacophore, both linked by a hydrazide bridge. The present study evaluates the ability of a novel chimeric peptide, AA501, to bind to opioid and substance P receptors and to produce antinociception in tail-flick and formalin tests, and in a neuropathic pain model when administered intrathecally to rats.

100 项与 AA-501 相关的药物交易

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