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计算机与应用化学 2002年第1期19卷 19-24页

作者：丁晓琴杨巨辉赵立峰邵华宙罗庆聪北京药物化学研究所北京102205

4-取代的咪唑类化合物是一类新发现的α2-受体肾上腺素能受体专一性激动剂,其代表物为medetomidine。medetomidine在一些国家已经作为动物麻醉药使用。本文用Catalyst软件包对这一系列的化合物进行了三维药效团模型研究,建立了与α1和... 详细信息

4-取代的咪唑类化合物是一类新发现的α2-受体肾上腺素能受体专一性激动剂,其代表物为medetomidine。medetomidine在一些国家已经作为动物麻醉药使用。本文用Catalyst软件包对这一系列的化合物进行了三维药效团模型研究,建立了与α1和α2-肾上腺素能受体结合的不同的药效团模型,2个模型的线性回归系数分别是0.96和0.99。通过建立的药效团模型,研究其结构与活性关系,以指导新的专一性α2-肾上腺素能受体激动剂的设计与合成。

关键词： medetomidine 类似物药效团模型 α2-肾上腺素能受体激动剂 Catalyst软件包麻醉镇痛药药物设计

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Electroencephalographic Recordings in the Canine: Effects of Low Dose medetomidine or Dexmedetomidine Followed by Atipamezole

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Open Journal of Veterinary Medicine 2014年第2期4卷 7-13页

作者： Laura C. Tepper Andy Shores Bay Street Animal Hospital Staten Island NY USA Veterinary Specialty Center Starkville MS USA College of Veterinary Medicine Mississippi State University Mississippi State MS USA

Objectives: 1) To describe electroencephalogram (EEG) appearance in the awake dog and compare these results with EEG recordings after low dose medetomidine (2 μg/kg IV) followed by atipamezole (10 μg/kg, IM);2) To institute EEG recordings after low dose medetomidine or dexmedetomidine as a standard of practice if focal abnormalities and amplitudes were not significantly altered by pharmaceuticals in Phase 1 of this study. Methods: Electroencephalograms were performed on eight clinical canine patients with suspected intracranial disease involving the prosencephalon. A five lead montage was used to record the EEGs. Each dog had an awake, baseline recording followed by an EEG performed after administration of low dose medetomidine (2 μg/kg IV) then atipamezole (10 μg/kg, IM). In the second phase of this study, the same dose of medetomidine or dexmedetomidine at 1 μg/kg IV and atipamezole (10 μg/kg, IM) were used in the evaluation of 20 clinical patients with suspected neurologic disease. Results: In Phase 1, awake recordings were laced with movement artifacts. After medetomidine and atipamezole, EEG waveforms were slower. Following atipamezole, however, the frequencies were observed to increase with time. Statistical evaluation revealed significantly more artifacts in baseline recordings. No statistically significant change was observed in focal abnormalities or amplitude. In Phase 2, the a2-adrenoreceptor agonists followed by atipamezole without the use of lidocaine produced clinically reliable results. Clinical Significance: Quality and diagnostic electroencephalogram (EEG) recordings are frequently inconvenient to obtain in the awake dog. Movement results in artifacts and dislodged leads. Administration of low dose medetomidine or dexmedetomidine followed by atipamezole reliably reduced the impact of movement artifacts and produced clinically valid EEG recordings in dogs.

关键词： Dog Brain Electroencephalogram medetomidine Atipamezole Dexmedetomidine

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Evaluation of cardiopulmonary effects of total intravenous anesthesia using a drug combination of medetomidine,lidocaine,butorphanol and propofol (MLBP-TIVA) with or without controlled ventilation and effect of positioning in mechanically ventilated horses

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畜牧与兽医 2012年第S2期44卷 35-35页

作者： Ishizuka T Nagaro T Sudo K Itami T Tamura J Fukui S Miyoshi K Yamashita K. Rakuno Gakuen University

The purpose of this study was to evaluate cardiopulmonary effects of MLBP-TIVA with or without controlled ventilation in horses and to determine effects of positioning on cardiovascular function in mechanically ventilated *** healthy adult horses were anesthetized with MLBP-TIVA for 2-hours on 3-occasions at 4-week interval with (CMV-group) or without controlled mechanical ventilation (SB-group) and in lateral (LR-group) or dorsal (DRgroup) *** was induced with lidocaine (1 mg/kg: IV) and propofol (3 mg/kg: IV) following premedications with medetomidine (0.005 mg/kg: IV) and butorphanol (0.02 mg/kg: IV),and then maintained by propofol infusion combined with constant rate infusions of medetomidine (0.0035 mg/kg/h),lidocaine (3 mg/kg/h)and butorphanol (0.024 mg/kg/h).Data were compared between groups using repeated-measures *** level of significance was set at P < *** parameters were maintained within acceptable ranges in ***,severe hypercapnia with insufficient oxygenation was observed (PaCO2: 83 ~103 mmHg,arterial O2pressure [PaO2]: 155 ~171 mmHg).In CMV-group,significant decreases in heart rate (29 ~ 31 beats/min,P = 0.020),cardiac output (17 ~ 21 L/min,P= 0.005) and PaCO2 (42 ~ 50 mmHg,P = 0.001) and a significant increase in PaO2 (395 ~ 419 mmHg,P =0.005) were observed compared to *** pulmonary arterial pressure and mean atrial blood pressure were significantly decreased in DR-group compared to LR-group (18 ~ 20 mmHg vs 27 ~ 31 mmHg,P = 0.001 and 8 ~ 9 mmHg vs 15 ~ 17 mmHg,P = 0.003,respectively).Arterial O2pressure was significantly lower in DR-group than in LR-group (171 ~301 mmHg vs 385 ~416 mmHg,P =0.043).Cardiovascular functions were maintained within acceptable range during MLBP-TIVA in *** ventilation is useful for improving hypercapnia and ***,MLBP-TIVA provides a preservation of cardiovascular function leading to compensation for decreased preload in hors

关键词： butorphanol cardiopulmonary effects horses lidocaine medetomidine propofol TIVA

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α2受体激动剂medetomidine

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世界临床药物 1988年第6期 358-359页

作者：杨爱民

合成咪唑-4-羧酸甲酯（Ⅰ）和2,3二甲基苯基镁溴（Ⅱ）在THF中经Grinard缩合得4-（2,3-二甲基苯甲酰）甲咪唑（Ⅲ）,再与甲基镁化碘（Ⅳ）在同样的溶剂中进行新的Grin-ard缩合得到1-（4-咪唑基）-1-（2,3-二甲基苯基）-乙醇（Ⅴ）,Ⅴ与... 详细信息

合成咪唑-4-羧酸甲酯（Ⅰ）和2,3二甲基苯基镁溴（Ⅱ）在THF中经Grinard缩合得4-（2,3-二甲基苯甲酰）甲咪唑（Ⅲ）,再与甲基镁化碘（Ⅳ）在同样的溶剂中进行新的Grin-ard缩合得到1-（4-咪唑基）-1-（2,3-二甲基苯基）-乙醇（Ⅴ）,Ⅴ与硫酸氢钾于136℃脱水得1-（4-咪唑基）-1-（2,3二甲基苯基）乙烯（Ⅵ）,Ⅵ最后在2 NHCl中经H2/Pd/C氢化即得本品[GB 2101114]。药理作用本品是一个选择性高的强效α2受体激动剂,与鸦片、腺甙、组胺或5-HT受体的亲和性很小或没有。大鼠脑放射性结

关键词：本品剂量用药量受体 medetomidine 激动剂

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