Effects of some antipsychotic drugs on cardiovascular catecholamine receptors in the rat.

M. Cuffí, E. Vila, A. Badía
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引用次数: 4

Abstract

1. Experiments were performed to determine the activity of four antipsychotic drugs on several catecholamine receptors that control the sympathetic cardiovascular responses in rats. 2. Chlorpromazine, thioridazine (0.03 and 0.1 mg kg-1) and haloperidol (0.3 and 1 mg kg-1) inhibited methoxamine-induced diastolic blood pressure increases in the pithed rat, whereas sulpiride (1 and 3 mg kg-1) was without effect. 3. Only sulpiride (3 mg kg-1) antagonized the pressor responses induced by xylazine. 4. Xylazine inhibited the heart rate increase induced by electrical stimulation of the spinal cord (C7-Th1) in the pithed rat. This effect was partially prevented by sulpiride (1 and 3 mg kg-1) and chlorpromazine (0.3 mg kg-1). A higher dose of chlorpromazine (1 mg kg-1) abolished the inhibitory effect of xylazine. 5. Apomorphine infusion inhibited the pressor responses induced by electrical stimulation (Th5-L4) in pithed rats. This effect was reversed by sulpiride (0.01, 0.03 and 0.1 mg kg-1) and partially antagonized by haloperidol (0.1 mg kg-1). 6. The depressor response to fenoldopam in anaesthetized rats was only inhibited by the higher dose of chlorpromazine and thioridazine (3 mg kg-1). 7. Our results suggest that, in the peripheral nervous system of the rat, haloperidol and sulpiride act as antagonists of DA2 receptors while chlorpromazine and thioridazine antagonized DA1 receptors. Furthermore, thioridazine and haloperidol show alpha 1-adrenoreceptor antagonist properties, whereas sulpiride antagonizes alpha 2-adrenoreceptors. Chlorpromazine shows mixed alpha 1/alpha 2-adrenoreceptor antagonism.
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一些抗精神病药物对大鼠心血管儿茶酚胺受体的影响。
1. 实验确定了四种抗精神病药物对控制大鼠交感心血管反应的几种儿茶酚胺受体的活性。2. 氯丙嗪、噻嗪(0.03和0.1 mg kg-1)和氟哌啶醇(0.3和1 mg kg-1)抑制甲氧嘧啶引起的舒张压升高,而舒匹利(1和3 mg kg-1)没有作用。3.只有舒必利(3mg kg-1)能拮抗噻嗪所致的升压反应。4. 二甲嗪抑制脊髓电刺激(C7-Th1)引起的心率升高。舒必利(1和3 mg kg-1)和氯丙嗪(0.3 mg kg-1)部分阻止了这种作用。较高剂量的氯丙嗪(1mg kg-1)可消除噻嗪的抑制作用。5. 阿波啡输注抑制电刺激大鼠的升压反应(Th5-L4)。舒必利(0.01、0.03和0.1 mg kg-1)可逆转这种作用,氟哌啶醇(0.1 mg kg-1)可部分拮抗这种作用。6. 麻醉大鼠对非诺多巴的抑制反应仅被较高剂量的氯丙嗪和硫硝嗪(3mg kg-1)所抑制。7. 我们的研究结果表明,在大鼠周围神经系统中,氟哌啶醇和舒必利是DA2受体的拮抗剂,而氯丙嗪和噻嗪则是DA1受体的拮抗剂。此外,硫硝嗪和氟哌啶醇显示α 1-肾上腺素受体拮抗剂特性,而舒必利拮抗α 2-肾上腺素受体。氯丙嗪具有α 1/ α 2-肾上腺素受体混合拮抗作用。
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