Simpkins J W, Bodor N, Enz A
J Pharm Sci. 1985 Oct;74(10):1033-6. doi: 10.1002/jps.2600741002.
Dopamine (1) was transformed into a lipoidal redox chemical delivery system which crosses the blood brain barrier and is converted to a quaternary ammonium precursor of 1, thus "locking in" this ionized moiety. Systemic administration of this chemical delivery system for 1 increased concentrations of the major acid metabolite of 1, dihydroxyphenylacetic acid, (6) in several brain regions, and despite sustained inhibition of prolactin secretion, concentrations of 1 were unchanged. Inhibition of monoamine oxidase did not encourage the formation of 1 from this delivery system. When de novo synthesis of 1 was inhibited, however, regional brain concentrations of both 1 and dihydroxyphenylacetic acid acid were increased by systemic administration of the delivery system. This study provides direct evidence for the brain-specific delivery of 1 by a redox chemical delivery system and indicates that the 1 formed is delivered to sites which normally store newly biosynthesized 1.
多巴胺（1）被转化为一种脂质氧化还原化学递送系统，该系统可穿过血脑屏障并转化为1的季铵前体，从而“锁定”这种离子化部分。对这种化学递送系统进行全身给药可增加1的主要酸性代谢物二羟基苯乙酸（6）在几个脑区的浓度，并且尽管催乳素分泌受到持续抑制，但1的浓度并未改变。单胺氧化酶的抑制并未促进该递送系统形成1。然而，当1的从头合成受到抑制时，通过该递送系统进行全身给药可增加脑区中1和二羟基苯乙酸的浓度。这项研究为氧化还原化学递送系统对1的脑特异性递送提供了直接证据，并表明所形成的1被递送至通常储存新生物合成的1的部位。
