在小鼠中,类固醇诱导的眼睛高血压通过选择性EP2,EP3,EP4和IP前列腺素受体激活剂以不同的方式降低
Najam A Sharif1,2,3,4,5,6,7,8, J Cameron Millar8, Gulab Zode9
1Ophthalmology Innovation Center, Santen Inc., Emeryville, CA 94608, USA.
International journal of molecular sciences
|March 28, 2024
概括
在小鼠模型中,五种前列腺素受体激活剂降低了眼内压力. 像mizoprostol和PF-04217329这样的EP2选择性激动剂证明了治疗眼睛高血压的最有效的IOP降低.
科学领域:
- 眼科医生 眼科 眼科
- 药理学 药理学是指药理学的学科.
- 药物发现 药物发现 药物发现
背景情况:
- 皮质类固醇诱导的眼睛高血压 (OHT) 是一个重大问题.
- 前列腺素 (PG) 受体激活剂正在研究用于控制眼内压力 (IOP).
研究的目的:
- 评估化学和代谢稳定的PG受体激动剂在甲诱导的OHT小鼠模型中的疗效.
- 为了比较不同PG受体激动剂之间IOP降低的开始和大小.
主要方法:
- 五种PG受体激动剂 (NS-304,rivenprost,mizoprostol,PF-04217329,butaprost) 的局部眼部注射每天两次,持续三周.
- 测量眼内压力 (IOP) 的变化.
- 对现有OHT治疗方法的文献调查.
主要成果:
- 所有测试的激动剂都显著降低了内压 (p < 0.05).
- 米索普罗斯托尔 (EP2/EP3/EP4) 和PF-04217329 (EP2) 显示出最快的开始时间和最大的疗效 (大约1. 减少了74%的IOP).
- 布塔普罗斯特 (EP2) 也显示出显著的疗效,而NS-304 (IP) 和rivenprost (EP4) 的疗效较慢.
结论:
- 选择性EP2前列腺素受体激动剂,如mizoprostol和PF-04217329,在治疗皮质类固醇诱导的眼睛高血压方面显示出有希望的疗效.
- 准EP2-PG受体可能是开发OHT新疗法的可行策略.
相关概念视频
Open Angle Glaucoma: Treatment
440
In open-angle glaucoma, the iridocorneal angle remains open, but the trabecular meshwork becomes stiff, slowing down the outflow of aqueous humor. This causes a buildup of aqueous humor in the anterior chamber, leading to a sudden increase in intraocular pressure. The treatment for open-angle glaucoma focuses on reducing the elevated intraocular pressure by either decreasing the secretion of aqueous humor or increasing its outflow.
Drugs such as carbonic anhydrase inhibitors, α2- and...
Drugs such as carbonic anhydrase inhibitors, α2- and...
440
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
173
Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
173


