Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography.

H Shinotoh, M Asahina, O Inoue, T Suhara, K Hirayama, Y Tateno
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引用次数: 13

Abstract

The effects of pharmacological intervention on brain muscarinic cholinergic receptor (mAChR) binding were assessed in seven patients with Parkinson's disease by positron emission tomography and carbon-11 labelled N-methyl-4-piperidyl benzilate ([11C]NMPB). [11C]NMPB was injected twice, approximately 2 hours apart, in each patient, to assess the effect of single doses of 4 mg of trihexyphenidyl (n = 5) or 400 mg of L-dopa with 57 mg of benserazide (n = 2) on the binding parameter of mAChRs (K3). There was a mean 28% inhibition of K3 values in the brain in the presence of trihexyphenidyl, which was assumed to reflect mAChR occupancy. No significant change in K3 was observed in the presence of L-dopa. This study demonstrates the feasibility of measuring mAChR occupancy by an anticholinergic medication with PET.

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正电子发射断层扫描测定三己苯和左旋多巴对脑毒菌碱胆碱能受体结合的影响。
通过正电子发射断层扫描和碳-11标记的n-甲基-4-哌啶苄酯([11C]NMPB)评估了7例帕金森病患者的药物干预对脑毒毒碱胆碱能受体(mAChR)结合的影响。[11C]在每位患者中注射两次NMPB,间隔约2小时,以评估单剂量4mg三苯基(n = 5)或400mg左旋多巴加57mg苯肼(n = 2)对machr结合参数(K3)的影响。在三己苯基的存在下,大脑中K3值的平均抑制率为28%,这被认为反映了mAChR的占用。左旋多巴对K3无明显影响。本研究证明了用PET测定抗胆碱能药物占用率的可行性。
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