BLOOD-BRAIN BARRIER - PENETRATION OF MORPHINE, CODEINE, HEROIN, AND METHADONE AFTER CAROTID INJECTION
BLOOD-BRAIN BARRIER - PENETRATION OF MORPHINE, CODEINE, HEROIN, AND METHADONE AFTER CAROTID INJECTION
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DOI：
10.1126/science.178.4064.984
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发表时间：
1972-01-01
期刊：
影响因子：
56.9
通讯作者：
HYMAN, S
中科院分区：
文献类型：
--
作者：
OLDENDORF, WH;OLDENDORF, SZ;HYMAN, S
将标记的吗啡、可待因、海洛因或美沙酮以推注形式注射到大鼠的颈总动脉中，15秒后将大鼠斩首。通过测量药物的脑含量作为同时注射的标记的、高度扩散的参考物质的百分比来计算药物的脑摄取。吗啡的摄取量低于可测量值；可待因的摄入率为 24%；海洛因，68%；和美沙酮，42%。还研究了静脉注射后吗啡和可待因的大脑摄取，并与颈动脉注射后的摄取密切相关。可待因的吸收在 30 秒内几乎完成。这些研究表明，大脑对某些药物的吸收非常快，静脉注射海洛因的吸收可能受到大脑局部血流的限制。讨论了海洛因快速渗透血脑屏障与其强烈成瘾特性的可能关系。
Labeled morphine, codeine, heroin, or methadone was injected as a bolus into the common carotid artery of the rat, and the rat was decapitated 15 seconds later. The brain uptake of the drug was calculated by measurement of the brain content of the drug as a percentage of a labeled, highly diffusible reference substance simultaneously injected. The uptake of morphine was below measurability; the uptake of codeine was 24 percent; heroin, 68 percent; and methadone, 42 percent. Brain uptakes of morphine and codeine were also studied after intravenous injection and correlated well with uptakes after carotid injection; the uptake of codeine being nearly complete by 30 seconds. These studies indicate that brain uptake of certain of these drugs is very rapid and that uptake of heroin injected intravenously is probably limited by the regional flow of blood in the brain. The possible relation of this rapid penetration of the blood-brain barrier by heroin to its strongly addictive properties is discussed.