6β-Naltrexol结构式
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常用名 | 6β-Naltrexol | 英文名 | 6β-Naltrexol |
|---|---|---|---|---|
| CAS号 | 49625-89-0 | 分子量 | 343.42 | |
| 密度 | 1.48g/cm3 | 沸点 | 557.5ºC at 760mmHg | |
| 分子式 | C20H25NO4 | 熔点 | 90-96ºC | |
| MSDS | N/A | 闪点 | 291ºC | |
| 符号 |
GHS02, GHS06, GHS08 |
信号词 | Danger |
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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 using B3LYP/6-31G** and SM5.4/A to estimate aqueous solvat... |
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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 longer duration of action largely attributed to 6-beta-nal... |
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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 the opioid receptor antagonist naltrexone and its metabolite... |
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Comparison of the opioid receptor antagonist properties of naltrexone and 6 beta-naltrexol in morphine-naïve and morphine-dependent mice.
Eur. J. Pharmacol. 583(1) , 48-55, (2008) It has been proposed that on chronic morphine treatment the micro-opioid receptor becomes constitutively active, and as a consequence, the opioid withdrawal response arises from a reduction in the level of this constitutively active receptor. In support of th... |
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An automated, highly sensitive LC-MS/MS assay for the quantification of the opiate antagonist naltrexone and its major metabolite 6beta-naltrexol in dog and human plasma.
J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 874(1-2) , 33-41, (2008) To support animal studies and clinical pharmacokinetic trials, we developed and validated an automated, specific and highly sensitive LC-MS/MS method for the quantification of naltrexone and 6beta-naltrexol in the same run. In human plasma, the assay had a lo... |
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Determination of naltrexone and 6beta-naltrexol in human blood: comparison of high-performance liquid chromatography with spectrophotometric and tandem-mass-spectrometric detection.
Anal. Bioanal. Chem 396(3) , 1249-57, (2010) We present data for a comparison of a liquid-chromatographic method coupled with tandem mass spectrometry (LC-MS/MS) and a high-performance liquid-chromatographic method with column switching and UV spectrophotometric detection. The two methods were developed... |
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The role of opioid antagonist efficacy and constitutive opioid receptor activity in the opioid withdrawal syndrome in mice.
Pharmacol. Biochem. Behav. 99(4) , 671-5, (2011) On the basis of efficacy, opioid antagonists are classified as inverse opioid agonists (e.g. naltrexone) or neutral opioid antagonists (e.g. 6β-naltrexol). This study examined the interaction between naltrexone and 6β-naltrexol in the precipitated opioid with... |
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Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
Bioorg. Med. Chem. Lett. 19(10) , 2811-4, (2009) Since the mu opioid receptor (MOR) is known to be involved in the therapeutically relevant pathways leading to the manifestation of pain and addiction, we are currently studying the specific structural characteristics that promote antagonism at the MOR. The o... |
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6beta-naltrexol preferentially antagonizes opioid effects on gastrointestinal transit compared to antinociception in mice.
Life Sci. 85(11-12) , 413-20, (2009) The current studies were designed to compare the in vivo potencies of the opioid antagonists 6beta-naltrexol and naltrexone in blocking the effects of the opioid agonist hydrocodone following intravenous (i.v.) or oral (p.o.) administration.Adult male CD-1 mi... |
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An efficient synthesis of 3-OBn-6β,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.
Bioorg. Med. Chem. Lett. 22(22) , 6801-5, (2012) In an effort to better understand the conformational preferences that inform the biological activity of naltrexone and related naltrexol derivatives, a new synthesis of the restricted analog 3-OBn-6β,14-epoxymorphinan 4 is described. 4 was synthesized startin... |