Mita H, Shida T
Allergy. 1983 Nov;38(8):547-52. doi: 10.1111/j.1398-9995.1983.tb04138.x.
Formoterol and salbutamol were compared for in vitro inhibition of allergen-induced histamine release from allergic leukocytes and human lung tissue passively sensitized with allergic serum. Formoterol inhibited the release of histamine from leukocytes but salbutamol showed little inhibiting effect. When combined with theophylline, formoterol was a more potent inhibitor of the release of histamine from leukocytes in allergic patients than salbutamol. In fragments of human lung sensitized with allergic serum, the concentration required to inhibit histamine release by 50% was 2 x 10(-11) M for formoterol and 8.5 x 10(-9) M for salbutamol. The potency of salbutamol and formoterol in blocking specific 3H-dihydroalprenolol binding to beta-adrenoceptors on guinea pig lung membranes revealed that formoterol had higher affinity for beta-adrenoceptors than salbutamol, and the concentration required for half-maximum stimulation of adenylate cyclase was approximately 200-fold higher for salbutamol than for formoterol.
对福莫特罗和沙丁胺醇进行了比较，观察它们在体外对变应原诱导的、来自经变应性血清被动致敏的变应性白细胞和人肺组织中的组胺释放的抑制作用。福莫特罗可抑制白细胞释放组胺，而沙丁胺醇的抑制作用很小。与茶碱合用时，在变应性患者中，福莫特罗对白细胞组胺释放的抑制作用比沙丁胺醇更强。在用变应性血清致敏的人肺组织切片中，福莫特罗抑制50%组胺释放所需的浓度为2×10⁻¹¹ M，沙丁胺醇为8.5×10⁻⁹ M。沙丁胺醇和福莫特罗阻断³H - 二氢阿普洛尔与豚鼠肺膜上β - 肾上腺素能受体特异性结合的效能表明，福莫特罗对β - 肾上腺素能受体的亲和力高于沙丁胺醇，沙丁胺醇使腺苷酸环化酶产生半最大刺激所需的浓度比对福莫特罗高约200倍。
