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源自大麻素的药物。7. Δ⁹-四氢大麻酚及一些合成类似物中的心动过速和镇痛构效关系。

Drugs derived from cannabinoids. 7. Tachycardia and analgesia structure-activity relationships in delta9-tetrahydrocannabinol and some synthetic analogues.

作者信息

Osgood P F, Howes J F, Razdan R K, Pars H G

出版信息

J Med Chem. 1978 Aug;21(8):809-11. doi: 10.1021/jm00206a018.

DOI:10.1021/jm00206a018
PMID:691006
Abstract

delta9-Tetrahydrocannabinol (delta9-THC) and eight other synthetic analogues were found to induce a dose-related increase in heart rate in the conscious Wistar rat. Ina comparison of tachycardia with analgesic activity (mouse hot-plate and antiwrithing tests) it was found that the water-soluble ester derivatives of 2a, 1-hydroxy-3-(3-methyl-2-octyl)-6,6,9-trimethyl-7,8,9,10-tetrahydro-6H-dibenzo(b,d)pyran (DMHP), had the least potency for tachycardia and the greatest potency for analgesia. These findings suggest that these compounds may have promise as therapeutic agents.

摘要

在清醒的Wistar大鼠中，发现Δ9-四氢大麻酚（Δ9-THC）和其他八种合成类似物会引起与剂量相关的心率增加。在将心动过速与镇痛活性（小鼠热板和抗扭体试验）进行比较时，发现2a，1-羟基-3-（3-甲基-2-辛基）-6,6,9-三甲基-7,8,9,10-四氢-6H-二苯并（b，d）吡喃（DMHP）的水溶性酯衍生物引起心动过速的效力最低，而镇痛效力最高。这些发现表明，这些化合物有望成为治疗药物。

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