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Cannabinoid-like effects of five novel carboxamide synthetic cannabinoids.
NeuroToxicology ( IF 3.4 ) Pub Date : 2018-11-12 , DOI: 10.1016/j.neuro.2018.11.004
Michael B Gatch 1 , Michael J Forster 1
Affiliation  

A new generation of novel cannabinoid compounds have been developed as marijuana substitutes to avoid drug control laws and cannabinoid blood tests. 5F-MDMB-PINACA (also known as 5F-ADB, 5F-ADB-PINACA), MDMB-CHIMICA, MDMB-FUBINACA, ADB-FUBINACA, and AMB-FUBINACA (also known as FUB-AMB, MMB-FUBINACA) were tested for in vivo cannabinoid-like effects to assess their abuse liability. Locomotor activity in mice was tested to screen for locomotor depressant effects and to identify behaviorally-active dose ranges and times of peak effect. Discriminative stimulus effects were tested in rats trained to discriminate Δ9-tetrahydrocannabinol (3 mg/kg, 30-min pretreatment). 5F-MDMB-PINACA (ED50 = 1.1 mg/kg) and MDMB-CHIMICA (ED50 = 0.024 mg/kg) produced short-acting (30 min) depression of locomotor activity. ADB-FUBINACA (ED50 = 0.19 mg/kg), and AMB- FUBINACA (ED50 = 0.19 mg/kg) depressed locomotor activity for 60-90 min; whereas MDMB-FUBINACA (ED50 = 0.04 mg/kg) depressed locomotor activity for 150 min. AMB-FUBINACA produced tremors at the highest dose tested. 5F-MDMB-PINACA (ED50 = 0.07), MDMB-CHIMICA (ED50 = 0.01 mg/kg), MDMB-FUBINACA (ED50 = 0.051 mg/kg), ADB-FUBINACA (ED50 = 0.075 mg/kg) and AMB-FUBINACA (ED50 = 0.029) fully substituted for the discriminative stimulus effects of Δ9-THC following 15-min pretreatment. All 5 compounds decreased locomotor activity and produced discriminative stimulus effects similar to those of Δ9-THC, which suggests they may have abuse liability similar to that of Δ9-THC. AMB-FUBINACA may have an increased risk of toxicities in recreational users.

中文翻译:

五个新型羧酰胺合成大麻素的类似大麻素的作用。

为了避免药物管制法和大麻素血液测试,已经开发了新一代新型大麻素化合物作为大麻替代品。测试了5F-MDMB-PINACA(也称为5F-ADB,5F-ADB-PINACA),MDMB-CHIMICA,MDMB-FUBINACA,ADB-FUBINACA和AMB-FUBINACA(也称为FUB-AMB,MMB-FUBINACA)对体内类大麻素作用进行评估,以评估其滥用责任。测试了小鼠的运动活动以筛选运动抑制作用并鉴定行为活性剂量范围和峰值作用时间。在受过训练以区分Δ9-四氢大麻酚(3 mg / kg,预处理30分钟)的大鼠中测试了歧视性刺激效果。5F-MDMB-PINACA(ED50 = 1.1 mg / kg)和MDMB-CHIMICA(ED50 = 0.024 mg / kg)导致运动活性的短时降低(30分钟)。ADB-FUBINACA(ED50 = 0.19 mg / kg),AMB-FUBINACA(ED50 = 0.19 mg / kg)运动能力降低60-90分钟;而MDMB-FUBINACA(ED50 = 0.04 mg / kg)会降低运动能力150分钟。AMB-FUBINACA在测试的最高剂量下会产生震颤。5F-MDMB-PINACA(ED50 = 0.07),MDMB-CHIMICA(ED50 = 0.01 mg / kg),MDMB-FUBINACA(ED50 = 0.051 mg / kg),ADB-FUBINACA(ED50 = 0.075 mg / kg)和AMB-FUBINACA (ED50 = 0.029)完全替代了15分钟预处理后Δ9-THC的歧视性刺激作用。所有5种化合物的运动能力降低,并产生与Δ9-THC相似的歧视性刺激作用,这表明它们可能具有与Δ9-THC相似的滥用责任。AMB-FUBINACA可能会增加娱乐用户的毒性风险。04 mg / kg)的运动能力降低,持续150分钟。AMB-FUBINACA在测试的最高剂量下会产生震颤。5F-MDMB-PINACA(ED50 = 0.07),MDMB-CHIMICA(ED50 = 0.01 mg / kg),MDMB-FUBINACA(ED50 = 0.051 mg / kg),ADB-FUBINACA(ED50 = 0.075 mg / kg)和AMB-FUBINACA (ED50 = 0.029)完全替代了15分钟预处理后Δ9-THC的歧视性刺激作用。所有5种化合物的运动能力降低,并产生与Δ9-THC相似的歧视性刺激作用,这表明它们可能具有与Δ9-THC相似的滥用责任。AMB-FUBINACA可能会增加娱乐用户的毒性风险。04 mg / kg)的运动能力降低,持续150分钟。AMB-FUBINACA在测试的最高剂量下会产生震颤。5F-MDMB-PINACA(ED50 = 0.07),MDMB-CHIMICA(ED50 = 0.01 mg / kg),MDMB-FUBINACA(ED50 = 0.051 mg / kg),ADB-FUBINACA(ED50 = 0.075 mg / kg)和AMB-FUBINACA (ED50 = 0.029)完全替代了15分钟预处理后Δ9-THC的歧视性刺激作用。所有5种化合物的运动能力降低,并产生与Δ9-THC相似的歧视性刺激作用,这表明它们可能具有与Δ9-THC相似的滥用责任。AMB-FUBINACA可能会增加娱乐用户的毒性风险。预处理15分钟后,ADB-FUBINACA(ED50 = 0.075 mg / kg)和AMB-FUBINACA(ED50 = 0.029)完全替代了Δ9-THC的歧视性刺激作用。所有5种化合物的运动能力降低,并产生与Δ9-THC相似的歧视性刺激作用,这表明它们可能具有与Δ9-THC相似的滥用责任。AMB-FUBINACA可能会增加娱乐用户的毒性风险。预处理15分钟后,ADB-FUBINACA(ED50 = 0.075 mg / kg)和AMB-FUBINACA(ED50 = 0.029)完全替代了Δ9-THC的歧视性刺激作用。所有5种化合物的运动能力降低,并产生与Δ9-THC相似的歧视性刺激作用,这表明它们可能具有与Δ9-THC相似的滥用责任。AMB-FUBINACA可能会增加娱乐用户的毒性风险。
更新日期:2018-11-12
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