Feigenbaum J J, Yanai J, Blass R B, Moon B, Klawans H
Pharmacol Biochem Behav. 1982 Feb;16(2):235-40. doi: 10.1016/0091-3057(82)90154-x.
Drugs that increase or decrease striatal dopamine levels appear to affect apomorphine induced stereotypy. This finding was unexpected, as it has previously been maintained that drugs which exert any action on striatal DA terminals exclusively would affect only indirect dopaminergic agonists, as opposed to apomorphine which induces stereotypy by acting directly on postsynaptic dopamine receptors. Specifically, inhibiting intrastriatal dopamine levels inhibits this behavior. This effect is explained in terms of apomorphine having a greater intrinsic activity and agonist affinity for striatal dopamine receptors than dopamine itself. Thus, dopamine and drugs which promote its release, may diminish the central behavioral effects induced by apomorphine relative to drugs which inhibit dopamine release centrally.
增加或降低纹状体多巴胺水平的药物似乎会影响阿扑吗啡诱导的刻板行为。这一发现出人意料,因为此前一直认为,仅对纹状体多巴胺末梢产生任何作用的药物只会影响间接多巴胺能激动剂,与通过直接作用于突触后多巴胺受体诱导刻板行为的阿扑吗啡不同。具体而言,抑制纹状体内多巴胺水平会抑制这种行为。这种效应可以用阿扑吗啡对纹状体多巴胺受体具有比多巴胺本身更大的内在活性和激动剂亲和力来解释。因此,多巴胺和促进其释放的药物,相对于在中枢抑制多巴胺释放的药物,可能会减弱阿扑吗啡诱导的中枢行为效应。