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Evidence that L-deprenyl treatment for one week does not inhibit MAO A or the dopamine transporter in the human brain

机译:L-异戊二烯治疗1周不会抑制人脑中的MAO A或多巴胺转运蛋白的证据

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In this study, we investigated whether treatment with L-deprenyl, a selective monoamine oxidase B (MAO B) inhibitor, also inhibits MAO A or the dopamine transporter in the human brain. Six normal volunteers (age 46 +/- 6 yrs) had two PET sessions, one at baseline and one following L-deprenyl (10 mg/day) for 1 week. Each session included one scan with [C-11]clorgyline (to assess MAO A) and one scan 2 hours later with [C-11]cocaine (to assess dopamine transporter availability). A 3-compartment model was used to compare the plasma-to-brain transfer constant, K, (a:function of blood flow) and Xk, (a kinetic term proportional to brain MAO A) before and after treatment. Dopamine transporter availability was measured as the ratio of distribution volumes of the striatum to cerebellum (DVR) which is equal to Bmax/K-D + 1. L-Deprenyl treatment for 1 week did not affect either brain MAO A activity or dopamine transporter availability. There was a non-significant trend for an increase in K, after L-deprenyl. These results confirm that L-deprenyl after one week of treatment at doses typically used clinically is selective for MAO B and that it does not produce a measurable affect on the dopamine transporter, suggesting that MAO A inhibition and dopamine transporter blockade do not contribute tb its pharmacological effects. (C) 2001 Elsevier Science Inc. All rights reserved. [References: 48]
机译:在这项研究中,我们调查了选择性单胺氧化酶B(MAO B)抑制剂L-异戊烯基的治疗是否还能抑制人脑中的MAO A或多巴胺转运蛋白。六名正常志愿者(年龄46 +/- 6岁)进行了两次PET治疗,一次在基线阶段,另一次在L-异戊二烯基(10毫克/天)治疗1周。每次会议包括一次用[C-11]氯胆碱扫描(以评估MAO A)和一次在2小时后用[C-11]可卡因扫描(以评估多巴胺转运蛋白的可用性)。使用三室模型比较治疗前后的血浆到大脑的转移常数K(a:血流量的函数)和Xk(与大脑MAO A成比例的动力学项)。多巴胺转运蛋白的可用性以纹状体与小脑(DVR)的分布体积之比等于Bmax / K-D + 1的方式进行测量。L-异戊二烯治疗1周对脑MAO A活性或多巴胺转运蛋白的可用性均无影响。在L-异戊二烯基之后,钾的增加没有显着趋势。这些结果证实,L-异戊二烯在临床上通常使用的剂量下治疗一周后对MAO B具有选择性,并且对多巴胺转运蛋白没有产生可测量的影响,这表明MAO A的抑制作用和多巴胺转运蛋白的阻滞作用对MAO B并无贡献。药理作用。 (C)2001 Elsevier Science Inc.保留所有权利。 [参考:48]

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