Medetomidine — a novel α2-adrenoceptor agonist: A review of its pharmacodynamic effects
Medetomidine — a novel α2-adrenoceptor agonist: A review of its pharmacodynamic effects
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美托咪定——一种新型α2-肾上腺素受体激动剂：药效学作用综述
DOI：
10.1016/0278-5846(89)90051-1
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发表时间：
1989
影响因子：
5.6
通讯作者：
M. Scheinin
中科院分区：
文献类型：
--
作者：
H. Scheinin;R. Virtanen;E. Macdonald;R. Lammintausta;M. Scheinin
1.本文综述了新型α 2肾上腺素受体激动剂美托咪定的药效学作用。2.在受体结合实验和离体器官制备中，美托咪定显示出对α 2-肾上腺素受体的高度特异性和选择性。其α 2/α 1选择性比为1620，而可乐定为220。它是α 2-肾上腺素受体的高效完全激动剂，这也是它与可乐定的区别。3.美托咪定可诱导去甲肾上腺素（NE）的中枢释放和转换呈剂量依赖性降低，通过代谢物浓度变化或使用药理学干预技术进行测量。4.美托咪定的选择性、特异性和效价得到了各种体内实验的进一步支持，这些实验显示了剂量依赖性消肿、心动过缓、镇静、抗焦虑、散瞳、体温过低和镇痛作用。5.美托咪定的药理学、神经化学和行为作用可以通过事先、同时或随后给予选择性和特异性α 2-拮抗剂来抑制。6.在人体中，美托咪定的耐受性良好，药效学作用（包括例如剂量依赖性降低警惕性、血压、心率、唾液分泌和血浆NE）与α 2-肾上腺素受体的激动作用一致。
1. The pharmacodynamic effects of medetomidine, a novel alpha 2-adrenoceptor agonist, are reviewed. 2. In receptor binding experiments, and in isolated organ preparations medetomidine shows high specificity and selectivity to alpha 2-adrenoceptors. Its alpha 2/alpha 1 selectivity ratio is 1620 compared to 220 of clonidine. It is a highly potent full agonist at alpha 2-adrenoceptors, a fact that also distinguishes it from clonidine. 3. Medetomidine induces a dose-dependent decrease in the central release and turnover of norepinephrine (NE) measured as changes in metabolite concentrations or using pharmacological intervention techniques. 4. The selectivity, specificity and potency of medetomidine is further supported by various in vivo experiments showing dose-dependent hypotensive, bradycardic, sedative, anxiolytic mydriatic, hypothermic and analgesic effects. 5. The pharmacological, neurochemical and behavioral effects of medetomidine can be inhibited by prior, simultaneous or subsequent administration of selective and specific alpha 2-antagonists. 6. In humans medetomidine is well-tolerated and pharmacodynamic effects including eg dose-dependent decrease of vigilance, blood pressure, heart rate, salivary secretion and plasma NE are compatible with an agonistic action at alpha 2-adrenoceptors.
去甲肾上腺素能调节血清素合成和代谢。
DOI：
--
发表时间：
1982
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
ReinhardJr,JF;Roth,RH
通讯作者：
Roth,RH
可乐定和灵长类蓝斑：证据表明具有抗焦虑和抗戒断作用。
DOI：
--
发表时间：
1981
期刊：
Progress in clinical and biological research
影响因子：
--
作者：
RedmondJr,DE
通讯作者：
RedmondJr,DE