Rudolphi K A, Schubert P
Hoechst Marion Roussel, Frankfurt/Main, Germany.
Behav Brain Res. 1997 Feb;83(1-2):123-8. doi: 10.1016/s0166-4328(97)86055-x.
Dementia is one of the major medical challenges in the industrialized countries. An increasing number of demented patients shows ischemic brain lesions. One strategy to treat dementia could be the reinforcement of the multifarious neuroprotective actions of the endogenous cell modulator adenosine. This involves the modulation of neuronal and glial cell functions. Adenosine appears to raise the threshold for the initiation of the pathophysiological cascade of ischemic neuronal death by counteracting ischemic membrane depolarization and the successive disturbance of intracellular Ca2+ homeostasis. When this threshold is overcome, adenosine seems to stimulate astrocyte differentiation and reinforce important protective astrocyte functions, e.g., synthesis and release of neurotrophic factors such as NGF and the clearance of abnormal neurotoxic levels of K+ and glutamate from the extracellular space. Propentofylline, a combined inhibitor of adenosine reuptake and cAMP phosphodiesterases, reinforces the actions of endogenous adenosine and cAMP. One important action of propentofylline is the inhibition of potentially neurotoxic functions of activated microglia (free radical formation and transformation into brain macrophages). Such drugs may help to inhibit the progressive neurodegenerative process in dementia.
痴呆症是工业化国家面临的主要医学挑战之一。越来越多的痴呆患者出现缺血性脑损伤。治疗痴呆症的一种策略可能是增强内源性细胞调节剂腺苷的多种神经保护作用。这涉及对神经元和神经胶质细胞功能的调节。腺苷似乎通过抵消缺血性膜去极化和随后细胞内Ca2+稳态的紊乱,提高缺血性神经元死亡病理生理级联反应起始的阈值。当这个阈值被突破时,腺苷似乎会刺激星形胶质细胞分化并增强重要的星形胶质细胞保护功能,例如神经营养因子如NGF的合成和释放,以及从细胞外空间清除异常神经毒性水平的K+和谷氨酸。丙戊茶碱是腺苷再摄取和cAMP磷酸二酯酶的联合抑制剂,可增强内源性腺苷和cAMP的作用。丙戊茶碱的一个重要作用是抑制活化小胶质细胞的潜在神经毒性功能(自由基形成和转化为脑巨噬细胞)。这类药物可能有助于抑制痴呆症中进行性神经退行性过程。