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大麻的镇静活性与其Δ'-反式-四氢大麻酚和大麻二酚含量的关系。

Sedative activity of cannabis in relation to its delta'-trans-tetrahydrocannabinol and cannabidiol content.

作者信息

Pickens J T

出版信息

Br J Pharmacol. 1981 Apr;72(4):649-56. doi: 10.1111/j.1476-5381.1981.tb09145.x.

DOI:10.1111/j.1476-5381.1981.tb09145.x
PMID:6269680
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2071638/
Abstract
  1. The oral sedative potencies of cannabis herb, crude ethanolic and petroleum-ether fractions, were assayed against delta'-trans-tetrahydrocannabinol (THC) administered orally to mice, by measuring spontaneous motor activity over 30 min periods, at selected times, up to 6 h. 2. The THC contents of the extracts were determined chemically by gas-liquid chromatography analysis and the B/C ratio (biological activity divided by chemical activity) calculated for each. The B/C values for cannabis herb, which contained THC but no CBD, was 4.47 and for ethanolic and petroleum-ether extracts, 5.26 and 4.39, respectively. 3. The sedative potency expressed as SDA50, the dose required to give 50% effect over 6 h, was 1.06 (0.98 to 1.15) mg/kg for THC; 4.72 (4.22 to 5.27) mg/kg for cannabidiol and 1.26 (1.22 to 1.80) mg/kg for chlorpromazine. 4. An infusion of cannabis herb made with boiling water was shown to have sedative activity of very low potency. 5. When the cannabinoids were completely extracted from a sample of herb with petroleum-ether the aqueous and ethanolic extracts of the marc had some sedative activity; but the 70% ethanolic fraction had none. 6. The sedative activity of THC, cannabis herb and a water soluble fraction is blocked by aspirin, a cyclo-oxygenase inhibitor, and restored by prostaglandin E2 (PGE2). 7. The sedative effect of chlorpromazine is not blocked by aspirin.
摘要
  1. 通过在长达6小时的选定时间内测量小鼠30分钟时间段的自发运动活性,对大麻草、乙醇粗提物和石油醚提取物的口服镇静效力进行了测定,以口服给予小鼠的δ'-反式-四氢大麻酚(THC)为对照。2. 通过气液色谱分析化学测定提取物中的THC含量,并计算每种提取物的B/C比值(生物活性除以化学活性)。不含大麻二酚(CBD)但含有THC的大麻草的B/C值为4.47,乙醇提取物和石油醚提取物的B/C值分别为5.26和4.39。3. 以SDA50表示的镇静效力,即6小时内产生50%效应所需的剂量,THC为1.06(0.98至1.15)mg/kg;大麻二酚为4.72(4.22至5.27)mg/kg,氯丙嗪为1.26(1.22至1.80)mg/kg。4. 用沸水冲泡的大麻草浸液显示出非常低的镇静活性。5. 当用石油醚从一份草样中完全提取大麻素时,残渣的水提取物和乙醇提取物具有一定的镇静活性;但70%乙醇馏分没有。6. THC、大麻草和一种水溶性馏分的镇静活性被环氧化酶抑制剂阿司匹林阻断,并被前列腺素E2(PGE2)恢复。7. 氯丙嗪的镇静作用不被阿司匹林阻断。

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本文引用的文献

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Pharmacological properties of thalidomide (alpha-phthalimido glutarimide), a new sedative hypnotic drug.新型镇静催眠药物沙利度胺(α-邻苯二甲酰亚胺戊二酰亚胺)的药理特性
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