CHRONIC CAFFEINE CONSUMPTION INCREASES THE NUMBER OF BRAIN ADENOSINE RECEPTORS
CHRONIC CAFFEINE CONSUMPTION INCREASES THE NUMBER OF BRAIN ADENOSINE RECEPTORS
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DOI：
10.1016/0024-3205(83)90119-4
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发表时间：
1983-01-01
期刊：
影响因子：
6.1
通讯作者：
MARANGOS, PJ
中科院分区：
文献类型：
--
作者：
BOULENGER, JP;PATEL, J;MARANGOS, PJ
咖啡因是一种强有力的中枢兴奋剂，在体外竞争性抑制腺苷和苯二氮卓受体配体与脑细胞膜的特异性结合。在小鼠中接受含有无毒剂量咖啡因的饮食（200或400 mg/kg饮食）长达40天，在全脑膜中观察到[3 H]CHA [环己基腺苷]和[3 H]DPX [1，3-二乙基-8-苯基黄嘌呤]结合位点数量的剂量相关性增加，而受体亲和力未发生变化。观察到[3 H]DZP结合位点的数量暂时增加。显然，腺苷受体参与咖啡因的作用模式，并可能与对该化合物的某些中枢作用的耐受性和依赖性的发展有关。
Caffeine, a potent central stimulant, competitively inhibits the specific binding of both adenosine and benzodiazepine receptor ligands to brain membranes in vitro. In mice receiving a diet containing nontoxic doses of caffeine (200 or 400 mg/kg diet) for periods up to 40 days, a dose-related increase in the number of binding sites for [3H]CHA [cyclohexyladenosine] and [3H]DPX [1,3-diethyl-8-phenylxanthine] was observed in whole brain membranes without modifications of the receptors'' affinity. A transitory increase in the number of [3H]DZP binding sites was observed. Evidently, the adenosine receptors are involved in the mode of action of caffeine and may be relevant to the development of both tolerance and dependence to some of the central effects of this compound.