Ganz A J, Waser P G
Arzneimittelforschung. 1980;30(3):471-7.
A series of synthetic cannabinoids were tested in mice for analgesic, anticonvulsant, sedative and reserpine antagonistic properties as well as for influence on body temperature and on motor coordination and compared with the natural delta 9-tetrahydrocannabinol (delta 9-THC), delta 8-tetrahydrocannabinol (delta 8-THC) and cannabidiol (CBD). All cannabinoids were injected s.c. or i.p. in mice as solutions in olive oil. The synthetic cannabinoids, with the exception of the lipophilic ones, were less active than the natural delta 9-THC. 1',1'-dimethyl-delta 8-tetrahydrocannabinol (DM-delta 8-THC) has an analgesic ED 50 of 16 mg/kg s.c. (writhing test) and is three times more active than delta 9-THC, but also eight times less active than morphine. The lipophilic derivatives of delta 8-THC prolonged pentobarbitone narcosis and diminished locomotor activity in mice. Anticonvulsant activities could never be detected; all cannabinoids slightly diminished body temperature and antagonized weakly the hypothermia induced by reserpine. The trained capacity of remaining on the rotating rod was severely shortened for a long time after application of all cannabinoids but mainly by the lipophilic ones. The influence of derivation on the activity of delta 9-THC is discussed.
对一系列合成大麻素进行了小鼠试验,以检测其镇痛、抗惊厥、镇静和利血平拮抗特性,以及对体温和运动协调性的影响,并与天然的δ9-四氢大麻酚(δ9-THC)、δ8-四氢大麻酚(δ8-THC)和大麻二酚(CBD)进行比较。所有大麻素均以橄榄油溶液的形式经皮下或腹腔注射给小鼠。除亲脂性大麻素外,合成大麻素的活性均低于天然的δ9-THC。1',1'-二甲基-δ8-四氢大麻酚(DM-δ8-THC)皮下注射(扭体试验)的镇痛半数有效剂量(ED50)为16mg/kg,活性是δ9-THC的三倍,但比吗啡低八倍。δ8-THC的亲脂性衍生物可延长小鼠戊巴比妥麻醉时间并降低其运动活性。未检测到抗惊厥活性;所有大麻素均轻微降低体温,并对利血平诱导的体温过低有微弱拮抗作用。应用所有大麻素后,尤其是亲脂性大麻素,小鼠在旋转杆上保持的训练能力在很长一段时间内严重缩短。文中讨论了衍生物对δ9-THC活性的影响。