Temple D L, Yevich J P, New J S
J Clin Psychiatry. 1982 Dec;43(12 Pt 2):4-10.
Buspirone is a lipophilic, dibasic heterocyclic with no structural resemblance to other anxiolytic or antipsychotic agents. Neurochemical binding studies suggest that buspirone has both dopamine agonist and antagonist properties. Structural comparisons with (+)-butaclamol indicate that buspirone possesses features required for binding at the postsynaptic dopamine receptor site. This is consonant with the drug's biologic properties, but does not define a mechanism for its anxioselective action. The transient antipsychotic effect associated with peak blood levels of buspirone in rats was consistent with such an effect, predicted by [3H]spiperone binding studies. The low (20 mg) anxioselective dose, acting in concert with extensive metabolism in humans, produces low blood levels of the parent drug, suggesting that buspirone's effect is exerted through interactions with a high-affinity, low-threshold receptor system.
丁螺环酮是一种亲脂性的二元杂环化合物，在结构上与其他抗焦虑药或抗精神病药没有相似之处。神经化学结合研究表明，丁螺环酮兼具多巴胺激动剂和拮抗剂的特性。与（+）-丁酰苯那嗪的结构比较表明，丁螺环酮具有在突触后多巴胺受体部位结合所需的特征。这与该药物的生物学特性相符，但并未明确其抗焦虑选择性作用的机制。大鼠体内与丁螺环酮血药浓度峰值相关的短暂抗精神病作用与[3H]螺哌隆结合研究预测的这种作用一致。低剂量（20毫克）的抗焦虑选择性作用，与人体广泛的代谢协同作用，使母体药物的血药浓度较低，这表明丁螺环酮的作用是通过与高亲和力、低阈值受体系统相互作用来发挥的。
