Neuropsychopharmacology Unit, Centre for Pharmacology and Therapeutics, Division of Experimental Medicine, Department of Medicine, Imperial College, London, United Kingdom.
Biol Psychiatry. 2012 Sep 1;72(5):371-7. doi: 10.1016/j.biopsych.2012.01.027. Epub 2012 Mar 3.
We aimed to demonstrate a pharmacologically stimulated endogenous opioid release in the living human brain by evaluating the effects of amphetamine administration on [(11)C]carfentanil binding with positron emission tomography (PET).
Twelve healthy male volunteers underwent [(11)C]carfentanil PET before and 3 hours after a single oral dose of d-amphetamine (either a "high" dose, .5 mg/kg, or a sub-pharmacological "ultra-low" dose, 1.25 mg total dose or approximately .017 mg/kg). Reductions in [(11)C]carfentanil binding from baseline to post-amphetamine scans (ΔBP(ND)) after the "high" and "ultra-low" amphetamine doses were assessed in 10 regions of interest.
[(11)C]carfentanil binding was reduced after the "high" but not the "ultra-low" amphetamine dose in the frontal cortex, putamen, caudate, thalamus, anterior cingulate, and insula.
Our findings indicate that oral amphetamine administration induces endogenous opioid release in different areas of human brain, including basal ganglia, frontal cortex areas, and thalamus. The combination of an amphetamine challenge and [(11)C]carfentanil PET is a practical and robust method to probe the opioid system in the living human brain.
我们旨在通过评估安非他命给药对正电子发射断层扫描（PET）中[（11）C]carfentanil 结合的影响，证明在活体人脑内存在药理学刺激内源性阿片释放。
12 名健康男性志愿者在单次口服安非他命（高剂量，0.5mg/kg，或亚药理超低剂量，总剂量 1.25mg 或约 0.017mg/kg）前后进行[（11）C]carfentanil PET。在“高”和“超低”安非他命剂量后，从基线到安非他命后扫描的[（11）C]carfentanil 结合减少（ΔBP（ND）），在 10 个感兴趣的区域进行评估。
在额皮质、纹状体、尾状核、丘脑、前扣带回和脑岛，“高”但不是“超低”安非他命剂量后，[（11）C]carfentanil 结合减少。
我们的发现表明，口服安非他命给药会导致人类大脑不同区域的内源性阿片释放，包括基底神经节、额皮质区和丘脑。安非他命挑战和[（11）C]carfentanil PET 的结合是一种实用且强大的方法，可以在活体人脑内探测阿片系统。
