Topical medication for the posterior part of the eye. The principles and the investigation of efficient drugs

用于眼睛后部的局部药物。

• 批准号: 12557146
• 负责人: ARAIE Makoto
• 金额: $ 8.38万
• 依托单位: The University of Tokyo
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (B)
• 财政年份: 2000
• 资助国家: 日本
• 起止时间: 2000 至 2001
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-12557146/
• 关键词: iganidipine; nipradilol; lomeridine; betaxolol; endothelin; optic nerve head; autoradiography; neuroprotection; セミオ-トラジオグラム; 網膜血管経

(1) Topically applied iganidipine (a water-soluble calcium antagonist) and nipradilol (an alpha-beta antagonist with nitric oxide releasing effect) showed the effects of increasing circulation in the optic nerve head of rabbits.(2) Lomeridine (a calcium antagonist) and betaxolol (a beta antagonist with calcium antagonistic effect) showed neuroprotective effects on the retinal ganglion cells or Muller cells of rats.(3) In rabbits, topically applied iganidipine penetrated into the retinal surface with the concentration sufficient to exert the inhibiting effects of vascular constriction caused with endothlin-1.(4) Autoradiography studies showed that topically applied iganidipine or nipradilol penetrated into the posterior portion of eye or into peribulbar tissues with sufficient concentration.(5) Long-term topical application of nipradilol, betaxolol, or iganidipine showed increasing effects on the optic nerve head circulation of normal humans.

(1)局部应用伊加尼地平（一种水溶性钙拮抗剂）和尼普拉洛（一种具有一氧化氮释放作用的α-β拮抗剂）显示出增加兔视神经乳头循环的作用。(2)钙拮抗剂洛美利定和具有钙拮抗作用的β受体拮抗剂倍他洛尔对大鼠视网膜神经节细胞或Muller细胞具有神经保护作用。(3)在兔中，局部应用的伊加尼地平渗透到视网膜表面，浓度足以发挥内皮素-1引起的血管收缩的抑制作用。(4)放射自显影研究表明，局部应用的iganidipine或nipradilol渗透到眼后部分或眼球周围组织，具有足够的浓度。(5)长期局部应用尼普拉洛、倍他洛尔或伊加尼地平对正常人视神经头循环的影响增加。

项目成果

Mizuno K: "Neuroprotective effect and intraocular penetration of hiprodilol, a beta-blocker with nitric oxide donative action"Invest.Ophthalmol.Vis.Sci.. 42. 688-694 (2001)

Mizuno K：“希普地洛（一种具有一氧化氮供给作用的 β 受体阻滞剂）的神经保护作用和眼内渗透”Invest.Ophasemol.Vis.Sci.. 42. 688-694 (2001)

Mizuno K: "Neuroprotective effect and intraocular penetration of nipradilol, a beta-blocking with nitric oxide donative action"Invest. Ophthalmol Vis. Sci.. 42. 688-694 (2001)

Mizuno K：“尼普地洛（一种具有一氧化氮捐赠作用的β-阻滞剂）的神经保护作用和眼内渗透”研究。

Mizuno K, Koide T, Yoshimura M. Araie M: "Neuroprotective effect and intraocular penetration of nipradilol, a beta-blocker with nitric oxide donative action"Invest Ophthalmol Vis Sci. 42. 688-694 (2001)

Mizuno K、Koide T、Yoshimura M. Araie M：“尼普地洛（一种具有一氧化氮捐赠作用的 β 受体阻滞剂）的神经保护作用和眼内渗透”Invest Ophasemol Vis Sci。

Kanno M: "Effects of topical nipradilol, a beta blocking agent with alpha blocking and nitroglycerin-like activities, on intraocular pressure and aqueous dynamics in humans"Br. J. Ophthalmol. 84. 293-299 (2000)

Kanno M：“局部尼普地洛（一种具有 α 阻断和硝酸甘油样活性的 β 阻断剂）对人体眼内压和房水动力学的影响”Br。

Tamaki Y, Araie M, Tomita K. Nagahara M: "Effect of topical betaxolol on tissue circulation in the human optic nerve head"J Ocul Pharmacol Ther. 15. 313-321 (1999)

Tamaki Y、Araie M、Tomita K. Nagahara M：“局部倍他洛尔对人视神经乳头组织循环的影响”J Ocul Pharmacol Ther。