DBO-17(DBO-17) - 药物靶点：Opioid receptors_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Opioid receptors

作用机制

Opioid receptors激动剂(阿片样受体激动剂)

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

University of Cagliari

在研机构-

非在研机构

University of Cagliari

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 DBO-17 相关的临床结果

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100 项与 DBO-17 相关的转化医学

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100 项与 DBO-17 相关的专利（医药）

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1

项与 DBO-17 相关的文献（医药）

1997-10-28·Naunyn-Schmiedeberg's Archives of Pharmacology4区 · 医学

Antinociceptive action of DBO 17 and DBO 11 in mice: two 3,8 diazabicyclo (3.2.1.) octane derivates with selective μ opioid receptor affinity

4区 · 医学

Article

作者: Paola Fadda ; Silvia Tronci ; Daniela Barlocco ; W. Fratta ; Giorgio Cignarella

Two 3,8 diazabicyclo (3.2.1.) octane derivates, namely DBO 17 and DBO 11, were studied for the opioid-like activity. In the rat brain membrane preparation binding studies, DBO 17 and DBO 11 showed a high affinity and selectivity for the mu opioid receptor (Ki's: 5.1 and 25 nM, respectively). DBO 17 and DBO 11 inhibited the nociceptive response in the hot-plate test of mice with ED50 values of 0.16 mg/kg and 0.44 mg/kg, respectively. The antinociceptive action of both DBO 17 and DBO 11 was blocked by naloxone. Tolerance to the antinociceptive action of DBO 17 and DBO 11 was present after 13 and 7 days of repeated treatment, respectively. Both DBO 17 and DBO 11 were ineffective in morphine-tolerant mice and vice versa. Chronic treatments (three times daily for seven consecutive days) of DBO 17 and DBO 11 induced a naloxone-precipitated withdrawal syndrome in DBO 17 treated mice similar to that in morphine treated mice, whereas in DBO 11 treated mice abstinence signs were virtually absent. These results indicate an interesting pharmacological profile that suggests these compounds as possible new candidates for the clinical treatment of pain.

100 项与 DBO-17 相关的药物交易

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