Consroe P, Benedito M A, Leite J R, Carlini E A, Mechoulam R
Eur J Pharmacol. 1982 Sep 24;83(3-4):293-8. doi: 10.1016/0014-2999(82)90264-3.
In mice, running, clonic and tonic convulsions and lethality were assessed following transcorneal (electroshock) current or convulsant drugs, each administered alone and after cannabidiol (CBD) pretreatment. CBD prevented tonic convulsions caused by a convulsant current (CC) 99.99, and by the convulsant dose (CD) 99.99 values of gamma-aminobutyric acid (GABA) inhibitors, 3-mercaptoproprionic acid (3MPA), picrotoxin (PIC), isonicotinic acid hydrazine (INH), pentylenetetrazol (PTZ) and bicuculline (BIC). Rankorder potencies, based on the antitonic ED50 of CBD, were: 3MPA greater than PIC = current = PTZ = BIC. Further, CBD prevented 3MPA-induced lethality, but failed to prevent the occurrence of the other behavioral endpoints of the above treatments. CBD also failed to prevent convulsions and lethality caused by the CD 99.99 of strychnine, a glycine antagonist. The differential effects of CBD suggest that the cannabinoid acts to inhibit seizure spread in the CNS by an action on GABA, but not glycine, mechanisms.
在小鼠中,分别单独给予以及在大麻二酚(CBD)预处理后,给予经角膜(电休克)电流或惊厥药物,评估跑步、阵挛性和强直性惊厥以及致死率。CBD预防了由惊厥电流(CC)引起的强直性惊厥,预防率达99.99%,还预防了γ-氨基丁酸(GABA)抑制剂、3-巯基丙酸(3MPA)、印防己毒素(PIC)、异烟肼(INH)、戊四氮(PTZ)和荷包牡丹碱(BIC)的惊厥剂量(CD)99.99%值所引起的强直性惊厥。基于CBD的抗强直性半数有效剂量(ED50),效力排序为:3MPA大于PIC = 电流 = PTZ = BIC。此外,CBD预防了3MPA诱导的致死率,但未能预防上述治疗的其他行为终点的出现。CBD也未能预防由甘氨酸拮抗剂士的宁的CD 99.99所引起的惊厥和致死率。CBD的不同作用表明,大麻素通过作用于GABA而非甘氨酸机制来抑制中枢神经系统中的癫痫扩散。