Solanki V, Murray A W
J Invest Dermatol. 1978 Nov;71(5):344-6. doi: 10.1111/1523-1747.ep12529844.
Binding of the potent beta-adrenergic antagonist [125I]iodohydroxybenzylpindolol ([125I]IHYP) to particulate preparations from newborn mouse skin was characterized. A number of criteria were used to establish that binding occurred to specific, high affinity beta-adrenergic receptors in the skin preparations. Thus specific binding (that displaced by 10 micrometer concentrations of the beta-adrenergic antagonist (-)propranolol) reached equilibrium in 15--20 min, was saturable (ligand concentration for half-maximal saturation, 0.25 nM) and freely reversible. Stereoselectivity of binding was demonstrated by the observation that displacement of [125I]IHYP by (-)propranolol occurred at concentrations at least 100 times lower than with (+)isoproterenol. Displacement was also observed with the beta-adrenergic agonists (-)isoproterenol, (-)epinephrine and (-)norepinephrine, but not with the alpha-adrenergic antagonist phentolamine.
对强效β-肾上腺素能拮抗剂[125I]碘羟基苄基吲哚洛尔（[125I]IHYP）与新生小鼠皮肤微粒体制剂的结合特性进行了表征。采用了多项标准来确定在皮肤制剂中与特异性、高亲和力β-肾上腺素能受体发生了结合。因此，特异性结合（被10微摩尔浓度的β-肾上腺素能拮抗剂（-）普萘洛尔所取代）在15 - 20分钟内达到平衡，具有饱和性（半数最大饱和度时的配体浓度为0.25纳摩尔）且可自由逆转。（-）普萘洛尔对[125I]IHYP的取代作用在浓度上至少比（+）异丙肾上腺素低100倍，这一观察结果证明了结合的立体选择性。β-肾上腺素能激动剂（-）异丙肾上腺素、（-）肾上腺素和（-）去甲肾上腺素也能产生取代作用，但α-肾上腺素能拮抗剂酚妥拉明则不能。
