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Atipamezole is an α₂‐adrenoceptor antagonist with an imidazole structure. Receptor binding studies indicate that its affinity for α₂‐adrenoceptors and its α₂/α₁ selectivity ratio are considerably higher than those of yohimbine, the prototype α₂‐adrenoceptor antagonist. Atipamezole is not selective for subtypes of α₂‐adrenoceptors. Unlike many other α₂‐adrenoceptor antagonists, it has negligible affinity for 5‐HT_1A and I₂ bindings 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 α₂‐adrenoceptor agonists. Due to this property, atipamezole is commonly used …