选择性抑制剂butyrylcholinesterase:一个有效的替代治疗阿尔茨海默病?
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Giacobini E
选择性抑制剂butyrylcholinesterase:一个有效的替代治疗阿尔茨海默病?
衰老药物。2001;18 (12):891 - 8。
- PubMed ID
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11888344 (在PubMed]
- 文摘
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哺乳动物的大脑含有两种主要形式的胆碱酯酶(;痒):乙酰胆碱酯酶(疼痛)和butyrylcholinesterase(大餐)。两种形式的基因不同,结构和动力学。Butyrylcholine不是生理基质在哺乳动物大脑的功能大餐难以解释。在人类的大脑,大餐是发现在神经元和胶质细胞以及神经炎的斑块和神经元纤维缠结在阿尔茨海默病(AD)患者。虽然疼痛活动逐步减少在AD患者的大脑,大餐活动显示了一些增加。为了研究函数的大餐,我们灌注的大鼠大脑皮层选择性大餐抑制剂。我们发现,细胞外的乙酰胆碱水平增加了15倍从5 nmol / L - 75 nmol / L浓度,与小胆碱能对动物产生不良影响。根据这些数据,我们假定两个池混身起红疹;痒的在大脑中可能存在:一个主要神经和疼痛相关的;和一个依赖主要是胶质和大餐。两个池显示不同的动力学特性对监管的大脑中乙酰胆碱浓度和分离选择性抑制剂。 The recent development of highly selective BuChE inhibitors will allow us to test these new agents in patients with AD in order to find out whether or not they represent an advantage for the treatment of patients with AD as compared with selective (donepezil) or relatively non-selective (rivastigmine, galantamine) ChE inhibitors presently in use. The association between a BuChE-K variant and AD has not been confirmed in several studies. In conclusion, additional experimental and clinical work is necessary in order to elucidate the role of BuChE in normal brain function and in the brains of patients with AD. In the future, it may be possible that selective BuChE inhibitors will have a role in treatment of patients with advanced AD.