Bree F, el Tayar N, Van de Waterbeemd H, Testa B, Tillement J P
J Recept Res. 1986;6(5-6):381-409. doi: 10.3109/10799898609074821.
Interaction of several agonists and antagonists with the relevant beta receptor were studied in vitro using rat lung membranes as beta-adrenergic receptor source. The influence of temperature, between 4 degrees C and 37 degrees C, on the ability of beta-adrenergic agonists and antagonists to displace (-)-[125I]iodocyanopindolol from beta-adrenergic receptors was checked. Thermodynamic parameters were calculated from the Kj values thus obtained. Lipophilicity of the twenty molecules was also measured using a RP-HPLC method. The results obtained show: the density of receptors was not affected by the temperature but their affinity for the twenty agonists and antagonists increased with decreasing temperature; the binding of agonists is enthalpy driven while that of antagonists is entropy driven, with the exception of the lipophilic agonist dobutamine; a single relationship between entropy and lipophilicity exists for all twenty compounds and would suggest that molecular structure and physicochemical properties account for the thermodynamics of binding.
使用大鼠肺膜作为β-肾上腺素能受体来源，在体外研究了几种激动剂和拮抗剂与相关β受体的相互作用。检测了4℃至37℃之间的温度对β-肾上腺素能激动剂和拮抗剂从β-肾上腺素能受体置换（-）-[125I]碘氰吲哚洛尔能力的影响。根据由此获得的Kj值计算热力学参数。还使用反相高效液相色谱法测量了这二十种分子的亲脂性。获得的结果表明：受体密度不受温度影响，但其对这二十种激动剂和拮抗剂的亲和力随温度降低而增加；激动剂的结合由焓驱动，而拮抗剂的结合由熵驱动，但亲脂性激动剂多巴酚丁胺除外；所有二十种化合物的熵和亲脂性之间存在单一关系，这表明分子结构和物理化学性质决定了结合的热力学。
