6β-Naltrexol

6β-Naltrexol用途

6β-Naltrexol (6β-Hydroxynaltrexone) 是 Naltrexone 的主要代谢物,是一种外周选择性 opioid 拮抗剂。6β-Naltrexol 选择性抑制胃肠道阿片作用,抑制 Morphine 诱导的胃肠道转运减慢。

6β-Naltrexol名称

[ CAS 号 ]:
49625-89-0

[ 英文名 ]:
6β-Naltrexol

[英文别名 ]:

6β-Naltrexol生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

信号通路 >> 神经信号通路 >> 阿片受体

研究领域 >> 神经疾病

[参考文献]

[1]. Cone EJ, et al. Biosynthesis, isolation, and identification of 6-beta-hydroxynaltrexone, a major human metabolite of naltrexone. J Pharm Sci. 1975 Apr;64(4):618-21.

[2]. Yancey-Wrona J, et al. 6β-naltrexol, a peripherally selective opioid antagonist that inhibits morphine-induced slowing of gastrointestinal transit: an exploratory study. Pain Med. 2011 Dec;12(12):1727-37.

6β-Naltrexol物理化学性质

[ 密度 ]:
1.48g/cm3

[ 沸点 ]:
557.5ºC at 760mmHg

[ 熔点 ]:
90-96ºC

[ 分子式 ]:
C₂₀H₂₅NO₄

[ 分子量 ]:
343.42

[ 闪点 ]:
291ºC

[ 精确质量 ]:
343.17800

[ PSA ]:
73.16000

[ LogP ]:
1.25510

[ 折射率 ]:
1.719

6β-Naltrexol安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 危险品运输编码 ]:
UN1230 - class 3 - PG 2 - Methanol, solution

6β-Naltrexol文献

Conformational analysis of 6α- and 6β-naltrexol and derivatives and relationship to opioid receptor affinity.

J. Chem. Inf. Model. 52(2) , 391-5, (2012)

Naltrexol and its C₆ α and β desoxy, iodo, mesyl, tosyl, trifyl, dimethylcarbamyl, and diphenylcarbamyl derivatives were studied in their energy-minimized C ring chair-like and boat-like conformations...

In vivo evaluation of a transdermal codrug of 6-beta-naltrexol linked to hydroxybupropion in hairless guinea pigs.

Eur. J. Pharm. Sci. 33(4-5) , 371-9, (2008)

6-Beta-naltrexol is the major active metabolite of naltrexone, NTX, a potent mu-opioid receptor antagonist used in the treatment of alcohol dependence and opioid abuse. Compared to naloxone, NTX has a...

Comparison of naltrexone, 6alpha-naltrexol, and 6beta-naltrexol in morphine-dependent and in nondependent rhesus monkeys.

Psychopharmacology 195(4) , 479-86, (2008)

Some opioid receptor ligands that appear to be neutral antagonists can have inverse agonist activity under conditions of increased constitutive activity (e.g., agonist treatment).This study compared t...

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