Severne Y, Vauquelin G
Dienst Chemie der Proteinen, Vrije Universiteit Brussel, Belgium.
Arch Int Pharmacodyn Ther. 1988 Mar-Apr;292:122-30.
beta 1-Adrenergic receptors of turkey and beta 2-receptors of rat erythrocyte membranes were identified by (-)-[3H]-dihydroalprenolol ([3H]-DHA) binding. Treatment of these membranes with the reagent cyanogen bromide causes a concentration dependent decrease in the number of binding sites, without affecting the affinity of the tracer. Whereas inactivation of the beta 1-receptors is not affected by the pH (between pH 6 and 9), substantial inactivation of the beta 2-receptors takes place only under mild acidic conditions. The ability of CNBr (cyanogen bromide) to discriminate between both receptor subclasses at basic pH is also confirmed for rat heart membranes (beta 1-receptors), Friend erythroleukemia and S49 lymphoma cell membranes (beta 2-receptors).
通过(-)-[³H]-二氢阿普洛尔([³H]-DHA)结合鉴定了火鸡的β1-肾上腺素能受体和大鼠红细胞膜的β2-受体。用溴化氰试剂处理这些膜会导致结合位点数量呈浓度依赖性减少,而不影响示踪剂的亲和力。β1-受体的失活不受pH值(pH 6至9之间)的影响,而β2-受体的显著失活仅在轻度酸性条件下发生。对于大鼠心脏膜(β1-受体)、弗氏红白血病细胞和S49淋巴瘤细胞膜(β2-受体),溴化氰(CNBr)在碱性pH下区分这两种受体亚型的能力也得到了证实。