Wax M B, Molinoff P B, Alvarado J, Polansky J
Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104-6084.
Invest Ophthalmol Vis Sci. 1989 Jan;30(1):51-7.
The characterization of beta-adrenergic receptors on cultured human trabecular cells and trabecular meshwork from human autopsy eyes was carried out by radioligand binding utilizing (125I)-iodopindolol. In cultured cells, the observed binding of (125I)-iodopindolol was of high affinity (Kd = 43 pM) and saturable. Scatchard plots were linear and revealed a Bmax of 33 +/- 7 fmol/mg of protein. Competition studies with a series of agonists and antagonists revealed that human trabecular cells contain a single class of beta-adrenergic receptors of the beta 2 subtype. Similarly, the IC50 of ICI 89,406 (176 nM) in human trabecular meshwork from autopsy eyes supports the presence of beta 2-adrenergic receptors in this tissue.
利用(125I)-碘吲哚洛尔通过放射性配体结合法对培养的人小梁细胞以及取自人类尸检眼的小梁网中的β-肾上腺素能受体进行了表征。在培养细胞中,观察到的(125I)-碘吲哚洛尔结合具有高亲和力(Kd = 43 pM)且可饱和。Scatchard图呈线性,显示每毫克蛋白质的Bmax为33±7 fmol。一系列激动剂和拮抗剂的竞争研究表明,人小梁细胞含有一类单一的β2亚型β-肾上腺素能受体。同样,ICI 89,406(176 nM)在尸检眼的人小梁网中的IC50支持该组织中存在β2-肾上腺素能受体。