Bönöczk P, Gulyás B, Adam-Vizi V, Nemes A, Kárpáti E, Kiss B, Kapás M, Szántay C, Koncz I, Zelles T, Vas A
Chemical Works of Gedeon Richter Ltd., Budapest, Hungary.
Brain Res Bull. 2000 Oct;53(3):245-54. doi: 10.1016/s0361-9230(00)00354-3.
Vinpocetine (ethyl apovincaminate) discovered during the late 1960s has successfully been used in the treatment of central nervous system disorders of cerebrovascular origin for decades. The increase in the regional cerebral blood flow in response to vinpocetine administration is well established and strengthened by new diagnostical techniques (transcranial Doppler, near infrared spectroscopy, positron emission tomography). The latest in vitro studies have revealed the effect of the compound on Ca(2+)/calmodulin dependent cyclic guanosine monophosphate-phosphodiesterase 1, voltage-operated Ca(2+) channels, glutamate receptors and voltage dependent Na(+)-channels; the latest being especially relevant to the neuroprotective action of vinpocetine. The good brain penetration profile and heterogenous brain distribution pattern (mainly in the thalamus, basal ganglia and visual cortex) of labelled vinpocetin were demonstrated by positron emission tomography in primates and man. Multicentric, randomized, placebo-controlled clinical studies proved the efficacy of orally administered vinpocetin in patients with organic psychosyndrome. Recently positron emission tomography studies have proved that vinpocetine is able to redistribute regional cerebral blood flow and enhance glucose supply of brain tissue in ischemic post-stroke patients.
20世纪60年代末发现的长春西汀（乙基阿朴长春胺酸）已成功用于治疗脑血管源性中枢神经系统疾病数十年。长春西汀给药后局部脑血流量增加已得到充分证实，新的诊断技术（经颅多普勒、近红外光谱、正电子发射断层扫描）进一步强化了这一结论。最新的体外研究揭示了该化合物对钙/钙调蛋白依赖性环磷酸鸟苷磷酸二酯酶1、电压门控钙通道、谷氨酸受体和电压依赖性钠通道的作用；其中最后一项尤其与长春西汀的神经保护作用相关。正电子发射断层扫描在灵长类动物和人类中证实了标记长春西汀良好的脑渗透特性和异质性脑分布模式（主要在丘脑、基底神经节和视觉皮层）。多中心、随机、安慰剂对照的临床研究证明口服长春西汀对患有器质性精神综合征的患者有效。最近的正电子发射断层扫描研究证明，长春西汀能够在缺血性中风后患者中重新分配局部脑血流量并增加脑组织的葡萄糖供应。
