Elena P P, Moulin G, Lapalus P
Curr Eye Res. 1984 May;3(5):743-50. doi: 10.3109/02713688409065597.
To analyse the molecular mechanism of action of beta-adrenergic compounds in reducing the intraocular pressure, the binding of 125I-iodohydroxybenzylpindolol to bovine pigmented ciliary processes was studied. The binding was found to be highly specific, saturable, reversible and displayed stereospecificity. Only one class of binding sites was detected. Values for KD of 0.18 nM and 0.32 nM were derived from kinetic and equilibrium experiments, respectively. The total number of beta receptors was large : 1.28 pmoles/mg protein. Competitive inhibition of 125I-iodohydroxybenzylpindolol binding by agonists and antagonists revealed that the majority of beta receptors in bovine pigmented ciliary processes were of the beta 2 type. The pharmacological and biochemical characteristics of the binding of adrenergic drugs found in these membranes are consistent with a regulation of aqueous humor production by the beta adrenergic system.
为分析β-肾上腺素能化合物降低眼压的分子作用机制，研究了¹²⁵I-碘羟基苄基吲哚洛尔与牛色素性睫状体的结合情况。发现该结合具有高度特异性、可饱和性、可逆性并表现出立体特异性。仅检测到一类结合位点。分别从动力学和平衡实验得出的KD值为0.18 nM和0.32 nM。β受体总数较多：1.28皮摩尔/毫克蛋白。激动剂和拮抗剂对¹²⁵I-碘羟基苄基吲哚洛尔结合的竞争性抑制表明，牛色素性睫状体中的大多数β受体为β₂型。在这些膜中发现的肾上腺素能药物结合的药理和生化特性与β-肾上腺素能系统对房水生成的调节作用一致。
