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    • 1. 发明申请
    • THERAPEUTIC USE OF CALCIUM ENTRY BLOCKERS IN RETINAL OR OPTIC NERVE DYSFUNCTION
    • 钙进入阻滞剂在视神经或神经功能障碍中的治疗应用
    • WO1990006123A1
    • 1990-06-14
    • PCT/US1989005487
    • 1989-12-05
    • HOUSTON BIOTECHNOLOGY INCORPORATEDCROSSON, Craig, E.POTTER, David, E.
    • HOUSTON BIOTECHNOLOGY INCORPORATED
    • A61K31/66
    • A61K31/275A61K31/00A61K31/44A61K31/495A61K31/505A61K31/55A61K31/66
    • Ischemia or edema of the retina or optic nerve results in retinal dysfunction. This retinal dysfunction can be associated with the activation of calcium channels and/or excitatory amino acid receptors. The prophylactic or therapeutic administration of compounds to block these processes can ameliorate or prevent retinal dysfunction. These compounds include the classes of calcium channel antagonists. Therapeutic treatment with compounds include dihydropyridines and diphenylipiperazines as calcium channel antagonists. Such compounds also exhibit a prophylactic effect to ischemia and edema of the retina or optic nerve. Rat models are provided for screening compounds capable of ameliorating retinal dysfunction. Particularly, calcium entry blockers and excitatory amino acid antagonists can be screened and the host eyes examined for the effect of the drugs. The model animal is a rat having a salt-inducible retinal dysfunction and/or a retinal dysfunction as a result of vascular occlusion resulting in ischemia.
    • 视网膜或视神经缺血或水肿导致视网膜功能障碍。 这种视网膜功能障碍可以与钙通道和/或兴奋性氨基酸受体的激活相关。 阻止这些过程的化合物的预防或治疗性给药可以改善或预防视网膜功能障碍。 这些化合物包括钙通道拮抗剂类。 化合物的治疗性治疗包括二氢吡啶和二苯哌嗪作为钙通道拮抗剂。 这些化合物还对视网膜或视神经的缺血和水肿具有预防作用。 提供大鼠模型用于筛选能够改善视网膜功能障碍的化合物。 特别地,可以筛选钙进入阻滞剂和兴奋性氨基酸拮抗剂,并且主机眼睛检查药物的作用。 模型动物是由于导致缺血的血管闭塞而具有盐诱导性视网膜功能障碍和/或视网膜功能障碍的大鼠。