Trope G E, Clark B
Br J Ophthalmol. 1982 Dec;66(12):788-92. doi: 10.1136/bjo.66.12.788.
Beta adrenergic receptors from membrane fragments of pigmented sheep eyes were studied and characterised by ligand binding techniques after the removal of melanin. In a representative experiment the beta max (total number of beta receptors) was 394.9 fmol/mg protein. The receptor affinity (Ka) was 440 pM. The potency series of drugs to displace 125I-HYP from the receptors was timolol = (-) propranolol greater than (+) propranolol greater than salbutamol greater than practolol. beta 1 Receptors were not detected in the ciliary processes. beta 2 Receptors were the prominent adrenergic receptors present. The theory as to how beta blockers work in glaucoma, their site of action, and the potential role of beta 2 blockers for use in intraocular pressure control is discussed.
去除黑色素后,利用配体结合技术对有色绵羊眼膜碎片中的β-肾上腺素能受体进行了研究和表征。在一个代表性实验中,βmax(β受体总数)为394.9 fmol/mg蛋白质。受体亲和力(Ka)为440 pM。药物从受体上取代125I-HYP的效价顺序为噻吗洛尔=(-)普萘洛尔>(+)普萘洛尔>沙丁胺醇>普拉洛尔。在睫状突中未检测到β1受体。β2受体是主要存在的肾上腺素能受体。讨论了β受体阻滞剂在青光眼中的作用机制、作用部位以及β2受体阻滞剂在控制眼压方面的潜在作用。