Pyrolysis of UR-144, a synthetic cannabinoid, augments an affinity to human CB1 receptor and cannabimimetic effects in mice
Pyrolysis of UR-144, a synthetic cannabinoid, augments an affinity to human CB1 receptor and cannabimimetic effects in mice
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DOI：
10.2131/jts.42.335
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发表时间：
2017-06-01
影响因子：
2
通讯作者：
Numazawa, Satoshi
中科院分区：
文献类型：
--
作者：
Kaizaki-Mitsumoto, Asuka;Hataoka, Kyoko;Numazawa, Satoshi
药物滥用者最常吸食“草药香”作为香烟或使用吸烟工具吸入。吸烟可能导致药物热解并产生分解产物，其生物学效应从未研究过。已知合成大麻素UR-144经历热降解，产生开环异构体，所谓的UR-144降解物。本研究通过使用UR-144作为模型药物证明，燃烧UR-144的烟雾含有UR-144降解物。与UR-144相比，UR-144降解产物对人CB、受体的激动剂活性约高出4倍，并在小鼠中增强了低温和运动不能作用。这些结果表明，吸烟行为可能会增加某些合成大麻素的心理作用。
Drug abusers most often smoke 'herbal incense' as a cigarette or inhale it using a smoking tool. Smoking may cause pyrolysis of the drug and produce decomposed products of which biological effect has never been investigated. The synthetic cannabinoid UR-144 is known to undergo thermal degradation, giving a ring-opened isomer, so-called UR-144 degradant. The present study demonstrates by using UR-144 as a model drug that the smoke of burned UR-144 contains the UR-144 degradant. The UR-144 degradant showed approximately four fold higher agonist activity to human CB, receptor and augmented hypothermic and akinetic actions in mice compared to UR-144. These results indicate that smoking behavior may increase psychological actions of the certain synthetic cannabinoids.