EVIDENCE FOR 5-HT2 INVOLVEMENT IN THE MECHANISM OF ACTION OF HALLUCINOGENIC AGENTS
EVIDENCE FOR 5-HT2 INVOLVEMENT IN THE MECHANISM OF ACTION OF HALLUCINOGENIC AGENTS
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DOI：
10.1016/0024-3205(84)90436-3
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发表时间：
1984-01-01
期刊：
影响因子：
6.1
通讯作者：
MCKENNEY, JD
中科院分区：
文献类型：
--
作者：
GLENNON, RA;TITELER, M;MCKENNEY, JD
将22种精神活性药物（包括LSD、5-OMe DMT [5-甲氧基-N，N-二甲基色胺]和一系列苯烷基胺衍生物）对皮质5-HT 1和5-HT 2结合位点的亲和力（Ki值）与2种行为活性测量方法（大鼠）进行比较。在使用1-（2，5-二甲氧基-4-甲基苯基）-2-氨基丙烷（DOM）作为训练药物的刺激泛化测试中测定的这些药剂的5-HT 2结合亲和力和它们的ED 50值之间存在显著相关性（r = 0.938）。对于这些药物中的15种，其中人体数据可用，5-HT 2结合亲和力与其人体致幻效力之间也存在显著相关性（r = 0.924）。这些药物的作用机制可能涉及5-HT 2相关事件。
The affinities (Ki values) of 22 psycho-active agents, including LSD, 5-OMe DMT [5-methoxy-N,N-dimethyl tryptamine] and a series of phenalkylamine derivatives, for cortical 5-HT1 and 5-HT2 binding sites were compared with 2 measures of behavioral activity [in rats]. A significant correlation (r = 0.938) exists between the 5-HT2 binding affinities of these agents and their ED50 values as determined in tests of stimulus generalization using 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) as the training drug. For 15 of these agents where human data where available, a significant correlation (r = 0.924) also exists between 5-HT2 binding affinities and their human hallucinogenic potencies. The mechanism of action of these agents may involve 5-HT2-related events.