Chang R S, Lotti V J
Life Sci. 1983 May 30;32(22):2603-9. doi: 10.1016/0024-3205(83)90245-x.
The beta-adrenergic antagonist, [3H]-dihydroalprenolol ([3H] DHA), binds to membranes prepared from the rat vas deferens in a specific and saturable manner. Scatchard and Hill plot analysis indicates a single class of binding sites with no evidence of cooperative interactions. The specific binding sites have a high affinity (Kd = 0.3 nM) and a maximal occupancy estimated to be 460 fmoles [3H]-DHA bound/g wet tissue weight. Beta-adrenergic agonists and/or antagonists inhibit [3H]-DHA binding to rat vas deferens membranes in a stereospecific manner and with a relative order of potency expected for beta-adrenergic receptors of the beta2 subtype. The receptor affinities of various beta-adrenergic antagonists in the rat vas deferens determined using inhibition of [3H]-DHA binding correlated with their receptor affinities determined physiologically using antagonism of isoproterenol-induced inhibition of neurogenic contractions in-vitro.
β-肾上腺素能拮抗剂[³H]-二氢烯丙洛尔（[³H] DHA）以特异性和可饱和的方式与大鼠输精管制备的膜结合。Scatchard和Hill图分析表明存在一类单一的结合位点，没有协同相互作用的证据。特异性结合位点具有高亲和力（Kd = 0.3 nM），最大占有率估计为460 fmol [³H]-DHA结合/克湿组织重量。β-肾上腺素能激动剂和/或拮抗剂以立体特异性方式抑制[³H]-DHA与大鼠输精管膜的结合，且具有β2亚型β-肾上腺素能受体预期的相对效价顺序。使用[³H]-DHA结合抑制法测定的各种β-肾上腺素能拮抗剂在大鼠输精管中的受体亲和力，与其使用异丙肾上腺素诱导的体外神经源性收缩抑制的拮抗作用以生理学方法测定的受体亲和力相关。
