Disclosed herein are non-competitive NMDA receptor antagonists having chemical structures similar to that of phencyclidine (PCP). These antagonists contain a polycyclic ring structure in place of the cycloalkyl ring of PCP. The antagonists also differ from PCP in that they include an electron withdrawing group, a hydroxyl group, or an amine group at the para position of the phenyl ring. The antagonists disclosed herein are useful for treating or ameliorating a symptom of ailments associated with over excitation of cells (e.g., neurons) that express NMDA receptors. Examples of ailments that can be treated and for which symptoms can be ameliorated include epilepsy, neurodegenerative disease (e.g., Alzheimer's and Parkinson's diseases), drug addiction, neuropathic pain, and neuronal and glutamate-dependent tumors.
本文披露了一些非竞争性N
MDA受体
拮抗剂,其
化学结构类似于
苯环
环己基胺(P
CP)。这些
拮抗剂在P
CP的
环烷基环上具有多环环结构。这些
拮抗剂还不同于P
CP,因为它们在
苯环的对位上包含一个电子吸引基,一个羟基或一个胺基。本文披露的
拮抗剂可用于治疗或缓解与表达N
MDA受体的细胞(例如神经元)的过度兴奋相关的症状。可治疗和缓解症状的疾病包括癫痫,神经退行性疾病(例如阿尔茨海默病和帕
金森病),药物成瘾,神经病理性疼痛以及神经元和谷
氨酸依赖性肿瘤。