SELECTIVE DEPLETING EFFECT OF SYROSINGOPINE ON BRAIN CATECHOLAMINE LEVELS WITH RELATION TO MORPHINE ANALGESIA IN RAT
SELECTIVE DEPLETING EFFECT OF SYROSINGOPINE ON BRAIN CATECHOLAMINE LEVELS WITH RELATION TO MORPHINE ANALGESIA IN RAT
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DOI：
10.1016/0091-3057(76)90058-7
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发表时间：
1976-01-01
影响因子：
3.6
通讯作者：
NAGASAKI, N
中科院分区：
文献类型：
--
作者：
FURUKAWA, T;SANO, T;NAGASAKI, N
萝芙木生物碱对脑胺的消耗作用中，利血平最有效，瑞西那明次之，昔洛舍平（利血平的合成类似物）最弱。与去甲肾上腺素（NE）和血清素（5-HT）相比，服用昔洛舍平后，大脑多巴胺（DA）的减少程度较小，持续时间较短，而利血平则引起这些胺的显着且持久的减少。因此，给药后2-4天，昔洛舍平诱导脑NE和5-HT的消耗，而不改变脑DA含量。每天 2 mg/kg 重复给予昔洛舍平 2 或 4 天，会导致脑胺水平发生类似的变化。昔洛西平对脑胺的这种选择性消耗作用通过与双硫仑或镰刀菌酸（一种多巴胺β-羟化酶抑制剂）联合治疗而增强。在重复给予昔洛西平2 mg/kg、连续2天诱导脑胺选择性耗尽的情况下，吗啡的镇痛作用不受影响，而利血平和丁苯那嗪拮抗吗啡的镇痛作用，同时引起所有脑胺的耗尽。就吗啡产生镇痛的机制而言，脑 DA 可能比脑 NE 或 5-HT 更重要。
Reserpine was the most potent, rescinnamine the next and syrosingopine [a synthetic analog of reserpine] the weakest in the depleting effects on brain amines of rauwolfia alkaloids. After syrosingopine, brain dopamine (DA) was decreased to a smaller degree and with a shorter duration as compared with norepinephrine (NE) and serotonin (5-HT), whereas reserpine elicited a marked and long lasting reduction in these amines. Accordingly, syrosingopine induced a depletion of brain NE and 5-HT without alteration in brain DA content 2-4 days after administration. Repeated administrations of syrosingopine, 2 mg/kg daily for 2 or 4 days, resulted in similar alterations in brain amine levels. This selective depleting effect of syrosinopine on brain amines was potentiated by combined treatment with disulfiram or fusaric acid, a dopamine .beta.-hydroxylase inhibitor. Under the condition of selective depletion of brain amines induced by repeated administrations of syrosinopine, 2 mg/kg daily for 2 days, the analgesic action of morphine was not affected, whereas reserpine and tetrabenazine antagonized morphine analgesia, concomitant with inducing a depletion of all brain amines. Brain DA may be more important than brain NE or 5-HT with regard to the mechanisms by which morpine produces analgesia.