Jori A, Caccia S, Guiso G, Garattini S
Eur J Pharmacol. 1978 Dec 1;52(3-4):361-5. doi: 10.1016/0014-2999(78)90290-x.
p-Hydroxy-d-amphetamine (p-OHdA) penetrates the blood--brain barrier poorly, when given acutely or by repeated systemic treatments, or when formed by biotransformation from administered d-amphetamine. However its distribution is relatively selective as it accumulates in the striatum more than in the brainstem. The rate of disappearance also differs in the two areas, being slower in the striatum than in the brainstem. These findings suggest that p-OHdA might be stored in different compartments. To check whether p-OHdA specificially accumulated in nerve terminals, catecholaminergic nerve endings were destroyed with 6-hydroxydopamine (6-OHDA). It has been shown that p-HOdA accumulates much less in the striatum of 6-OHDA-treated rats than of controls. This effect was not present in the brainstem. Accumulation of p-OHdA was similar after repeated d-amphetamine administration. The results are interpreted as showing that p-OHdA tends to accumulate in dopaminergic structures.
对羟基 - d - 苯丙胺（p - OHdA）在急性给药、重复全身给药或由给药的d - 苯丙胺经生物转化形成时，穿透血脑屏障的能力较差。然而，其分布具有相对选择性，因为它在纹状体中的积累多于脑干。两个区域的消失速率也不同，纹状体中的消失速率比脑干中的慢。这些发现表明p - OHdA可能储存在不同的隔室中。为了检查p - OHdA是否特异性地积累在神经末梢，用6 - 羟基多巴胺（6 - OHDA）破坏儿茶酚胺能神经末梢。结果表明，与对照组相比，6 - OHDA处理的大鼠纹状体中p - HOdA的积累要少得多。这种效应在脑干中不存在。重复给予d - 苯丙胺后，p - OHdA的积累情况相似。这些结果被解释为表明p - OHdA倾向于在多巴胺能结构中积累。
