PH I STUDY TO ASSESS SAFETY & TOLERABILITY OF LICOSTINEL

中风是美国第三大死亡原因，也是导致严重残疾的头号原因。人们正在寻求新的方法来限制急性中风患者的神经损伤程度。其中一种方法是使用n -甲基-天冬氨酸（NMDA）受体拮抗剂。licostiel是一种选择性NMDA拮抗剂，似乎比以前测试的药物产生更少的中枢神经系统副作用。本研究的主要目的是确定probenecid对licostine药代动力学的影响。我们将确定licostel单独使用或与probenecid联合使用对licostel给药部位的肾功能和静脉炎症的影响。预期丙炔酸能显著延长利柯替尼的半衰期，减少利柯替尼由肾脏排出的量。在这项18例患者的研究中获得的信息将用于计划更明确的研究，并寻求确定利司替尼的最佳给药途径。

Stroke is the third largest cause of death and the number one cause of serious disability in the United States. New methods are being sought to limit the amount of neuronal damage that occurs in patients who have had an acute stroke. One of these methods is with a group of drugs that are antagonists of the N-methyl-Daspartate (NMDA) receptor. Licostinel is a selective NMDA antagonist that appears to produce fewer central nervous system side effects than previously tested agents. The principal objective of this study is to determine the effects of probenecid on the pharmacokinetic profile of licostinel. A determination will be made to seek the effects of licostinel when administered alone or in combination with probenecid on renal function and venous inflammation at the site of licostinel administration. It is expected that probenecid will markedly prolong the half life of licostinel and reduce the amount of licostinel that is excreted by the kidneys. Information obtained during this study of 18 patients will be used to plan more definitive studies and seek to determine an optimal route of licostinel administration.