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首页> 外文期刊>CNS drug reviews >Pharmacological properties, central nervous system effects, and potential therapeutic applications of atipamezole, a selective alpha2-adrenoceptor antagonist.
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Pharmacological properties, central nervous system effects, and potential therapeutic applications of atipamezole, a selective alpha2-adrenoceptor antagonist.

机译：选择性α2-肾上腺素能受体拮抗剂阿替帕唑的药理特性，中枢神经系统作用和潜在的治疗应用。

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Atipamezole is an alpha2-adrenoceptor antagonist with an imidazole structure. Receptor binding studies indicate that its affinity for alpha2-adrenoceptors and its alpha2/alpha1 selectivity ratio are considerably higher than those of yohimbine, the prototype alpha2-adrenoceptor antagonist. Atipamezole is not selective for subtypes of alpha2-adrenoceptors. Unlike many other alpha2-adrenoceptor antagonists, it has negligible affinity for 5-HT1A and I2 binding sites. Atipamezole is rapidly absorbed and distributed from the periphery to the central nervous system. In humans, atipamezole at doses up to 30 mg/subject produced no cardiovascular or subjective side effects, while at a high dose (100 mg/subject) it produced subjective symptoms, such as motor restlessness, and an increase in blood pressure. Atipamezole rapidly reverses sedation/anesthesia induced by alpha2-adrenoceptor agonists. Due to this property, atipamezole is commonly used by veterinarians to awaken animals from sedation/anesthesia induced by alpha2-adrenoceptor agonists alone or in combination with various anesthetics. Atipamezole increased sexual activity in rats and monkeys. In animals with sustained nociception, atipamezole increased pain-related responses by blocking the noradrenergic feedback inhibition of pain. In tests assessing cognitive functions, atipamezole at low doses has beneficial effects on alertness, selective attention, planning, learning, and recall in experimental animals, but not necessarily on short-term working memory. At higher doses atipamezole impaired performance in tests of cognitive functions, probably due to noradrenergic overactivity. Recent experimental animal studies suggest that atipamezole might have beneficial effects in the recovery from brain damage and might potentiate the anti-Parkinsonian effects of dopaminergic drugs. In phase I studies atipamezole has been well tolerated by human subjects.
机译：Atipamezole是具有咪唑结构的α2-肾上腺素能受体拮抗剂。受体结合研究表明，其对α2-肾上腺素受体的亲和力及其alpha2 /α1选择性比明显高于原型α2-肾上腺素受体拮抗剂育亨宾的亲和力。 Atipamezole对α2-肾上腺素受体的亚型没有选择性。与许多其他α2-肾上腺素受体拮抗剂不同，它对5-HT1A和I2结合位点的亲和力可忽略不计。 Atipamezole被迅速吸收并从周围分布到中枢神经系统。在人类中，阿帕米唑的最高剂量为30毫克/受试者，不会产生心血管或主观的副作用，而在高剂量（100毫克/受试者）下，它会产生主观症状，例如运动不安和血压升高。 Atipamezole可以迅速逆转由α2肾上腺素受体激动剂引起的镇静/麻醉作用。由于这种特性，兽医通常使用阿替哌唑来唤醒动物，使其免受单独或与多种麻醉剂结合使用的α2-肾上腺素受体激动剂引起的镇静/麻醉作用。 Atipamezole增加了大鼠和猴子的性活动。在具有持续伤害感受的动物中，阿替帕唑通过阻断去甲肾上腺素能反馈抑制疼痛而增加了与疼痛相关的反应。在评估认知功能的测试中，低剂量的安替他唑对实验动物的警觉性，选择性注意力，计划，学习和记忆有有益作用，但不一定对短期工作记忆有好处。在较高剂量下，阿替帕唑在认知功能测试中的表现受损，这可能是由于去甲肾上腺素过度活跃。最近的实验动物研究表明，阿帕米唑可能对脑损伤的恢复具有有益作用，并可能增强多巴胺能药物的抗帕金森病作用。在第一阶段的研究中，人类受试者对阿替哌唑的耐受性良好。

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