Darlington Cynthia L
University of Otago Medical School, Department of Pharmacology and Toxicology, Dunedin, New Zealand.
IDrugs. 2003 Oct;6(10):976-9.
Dexanabinol was developed as a synthetic analog of the cannabinoid tetrahydrocannabinol, however, the action of the drug is as a weak, uncompetitive antagonist at the N-methyl-D-aspartate (NMDA) receptor. Dexanabinol is an effective neuroprotectant in animal models of hypoxemia/ischemia, neurotoxin exposure and nerve crush. Unlike some other uncompetitive NMDA receptor antagonists, dexanabinol does not produce psychotrophic effects and is generally well tolerated in humans. In this respect it is similar to the uncompetitive NMDA receptor antagonist memantine. Dexanabinol is currently in phase III clinical trials for severe head injury. It is a promising drug that appears to be able to provide the therapeutic benefits of uncompetitive NMDA-receptor antagonists without the adverse side effects associated with some of the earlier drugs of this type.
右大麻酚是作为大麻素四氢大麻酚的合成类似物而研发的,然而,该药物的作用是作为N-甲基-D-天冬氨酸(NMDA)受体的一种弱非竞争性拮抗剂。右大麻酚在低氧血症/缺血、神经毒素暴露和神经挤压的动物模型中是一种有效的神经保护剂。与其他一些非竞争性NMDA受体拮抗剂不同,右大麻酚不会产生精神营养作用,并且在人类中通常耐受性良好。在这方面,它与非竞争性NMDA受体拮抗剂美金刚类似。右大麻酚目前正处于针对重度颅脑损伤的III期临床试验阶段。它是一种有前景的药物,似乎能够提供非竞争性NMDA受体拮抗剂的治疗益处,而没有与该类早期一些药物相关的不良副作用。