Masini E, Fantozzi R, Blandina P, Galli A, Bani-Sacchi T, Giotti A, Zilletti L, Mannaioni P F
Naunyn Schmiedebergs Arch Pharmacol. 1982 Dec;321(3):171-6. doi: 10.1007/BF00505481.
The correlation between the binding of a beta-adrenoceptor antagonist, (--)[3H]-dihydroalprenolol (DHAP), and the adrenergic inhibition of histamine release by acetylcholine and by compound 48/80 was studied with isolated purified rat mast cells and in rat mast cell crude membrane fractions. Acetylcholine-evoked histamine release was inhibited by catecholamines, in the order isoprenaline greater than adrenaline greater than noradrenaline. Pretreatment of cells with (--)alprenolol antagonized the inhibitory effect of isoprenaline on acetylcholine-induced histamine release. 40/80-evoked histamine release was blocked by isoprenaline at significantly higher concentrations than those required to inhibit cholinergic histamine release. The inhibitory effect of isoprenaline was equally antagonized by preincubating mast cells with (--)alprenolol. Specific binding sites for DHAP have been demonstrated in rat mast cell membranes. The specific binding of DHAP was inhibited by adrenoceptor agonists and antagonists according to the stereospecificity of these compounds. A close correlation between the binding-inhibitory potency of various adrenergic compounds and the data obtained in the pharmacological experiments was found, thus indicating the presence of beta-adrenoceptors in rat mast cells.
利用分离纯化的大鼠肥大细胞和大鼠肥大细胞粗膜组分，研究了β-肾上腺素能受体拮抗剂（-）[³H] - 二氢烯丙洛尔（DHAP）的结合与乙酰胆碱及化合物48/80对组胺释放的肾上腺素能抑制作用之间的相关性。儿茶酚胺可抑制乙酰胆碱诱发的组胺释放，其抑制顺序为异丙肾上腺素＞肾上腺素＞去甲肾上腺素。用（-）烯丙洛尔预处理细胞可拮抗异丙肾上腺素对乙酰胆碱诱导的组胺释放的抑制作用。与抑制胆碱能组胺释放所需浓度相比，异丙肾上腺素在显著更高浓度时可阻断化合物48/80诱发的组胺释放。用（-）烯丙洛尔预孵育肥大细胞，可同样拮抗异丙肾上腺素的抑制作用。已在大鼠肥大细胞膜中证实存在DHAP的特异性结合位点。根据这些化合物的立体特异性，肾上腺素能激动剂和拮抗剂可抑制DHAP的特异性结合。发现各种肾上腺素能化合物的结合抑制效力与药理实验所得数据之间存在密切相关性，从而表明大鼠肥大细胞中存在β-肾上腺素能受体。
