Nicergoline is a non-selective alpha-adrenergic receptor antagonist which can decrease vascular resistance and increase arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells.
Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. Nicergoline is a potent and selective alpha 1A-adrenoceptor subtype antagonist, an alpha 1-adrenoceptor subtype which is mainly represented in resistance arteries. Nicergoline displaced [3H]-prazosin bound to rat forebrain membranes pretreated with chloroethylclonidine (pKi = 9.9 +/- 0.2) at concentrations 60-fold lower than in rat liver membranes (pKi = 8.1 +/- 0.2)[3]. Nicergoline ameliorated apoptosis in hippocampal cells and hippocampus tissue in 3xTg-AD mice with Alzheimer's disease. In addition, the expression levels of inflammatory factors, in addition to oxidative stress, were decreased in hippocampal cells treated with nicergoline. Additionally, amyloid precursor protein accumulation was cleared in the hippocampal area in nicergoline-treated mice. Nicergoline inhibited neuronal loss and prevented cognitive impairment through the restoration of learning/memory ability[4]. Nicergoline treatment improves perfusion of the frontal and parietal regions in early AD patients. It is possible that the increased perfusion in the superior frontal gyrus may be related to the mechanisms that delay or prevent progressive deterioration of cognitive functions in AD[5].
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