大鼠脑尾状核中对多巴胺敏感的腺苷酸环化酶及其与“多巴胺受体”的相似性。
Dopamine-sensitive adenylate cyclase in caudate nucleus of rat brain, and its similarity to the "dopamine receptor".
作者信息
Kebabian J W, Petzold G L, Greengard P
出版信息
Proc Natl Acad Sci U S A. 1972 Aug;69(8):2145-9. doi: 10.1073/pnas.69.8.2145.
Abstract
An adenylate cyclase that is activated specifically by low concentrations of dopamine has been demonstrated in homogenates of caudate nucleus of rat brain. A half-maximal increase in the activity of the enzyme occurred in the presence of 4 muM dopamine. Concentrations of dopamine as low as 0.3 muM stimulated the activity of the enzyme. The adenylate cyclase activity of the homogenates was also stimulated by low concentrations of apomorphine, a substance known to mimic the physiological and pharmacological effects of dopamine. The stimulatory effect of dopamine was blocked by low concentrations of either haloperidol or chlorpromazine, agents known to block the actions of dopamine in mammalian brain. The results suggest that dopamine-sensitive adenylate cyclase may be the receptor for dopamine in mammalian brain. The isolation of this enzyme from caudate nucleus should facilitate the search for new therapeutic agents useful in the treatment of extrapyramidal diseases.
摘要
在大鼠脑尾状核匀浆中已证实有一种腺苷酸环化酶，它能被低浓度多巴胺特异性激活。在存在4μM多巴胺的情况下，该酶活性出现半数最大增加。低至0.3μM的多巴胺浓度就能刺激该酶的活性。低浓度的阿扑吗啡也能刺激匀浆的腺苷酸环化酶活性，阿扑吗啡是一种已知能模拟多巴胺生理和药理作用的物质。多巴胺的刺激作用被低浓度的氟哌啶醇或氯丙嗪阻断，这两种药物是已知能阻断多巴胺在哺乳动物脑中作用的药剂。结果表明，多巴胺敏感的腺苷酸环化酶可能是多巴胺在哺乳动物脑中的受体。从尾状核中分离出这种酶应有助于寻找用于治疗锥体外系疾病的新型治疗药物。
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