Rudd R M, Gellert A R, Studdy P R, Geddes D M
Br J Dis Chest. 1983 Jan;77(1):78-86.
M&B 22,948 (2-o-propoxyphenyl-8-azapurin-6-one) is an orally absorbed mast cell stabilizer which is 30 times as potent as disodium cromoglycate in laboratory and animal studies. In a double-blind placebo-controlled cross-over trial we studied the protection afforded by a single oral dose of 10 mg of M&B 22,948 against asthma induced by histamine and exercise, each in 12 patients. Compared with placebo the drug had no significant effect on the response to inhaled histamine but significantly inhibited the fall in FEV1 induced by exercise on treadmill (P less than 0.005). The exercise-induced fall in FEV1 was less following M&B 22,948 than placebo in all patients and the fall was inhibited by more than 50% in five (42%) of 12 patients. The degree of inhibition was significantly correlated with the plasma drug concentration (r = 0.65, P less than 0.025). M&B 22,948 merits evaluation in the treatment of asthma.
M&B 22,948(2-邻丙氧基苯基-8-氮杂嘌呤-6-酮)是一种口服吸收的肥大细胞稳定剂,在实验室和动物研究中其效力是色甘酸二钠的30倍。在一项双盲安慰剂对照交叉试验中,我们对12名患者分别给予单次口服10毫克M&B 22,948,研究其对组胺诱发哮喘和运动诱发哮喘的保护作用。与安慰剂相比,该药物对吸入组胺的反应无显著影响,但能显著抑制跑步机运动诱发的第一秒用力呼气容积(FEV1)下降(P<0.005)。在所有患者中,服用M&B 22,948后运动诱发的FEV1下降幅度均小于服用安慰剂,12名患者中有5名(42%)下降幅度被抑制超过50%。抑制程度与血浆药物浓度显著相关(r = 0.65,P<0.025)。M&B 22,948值得在哮喘治疗中进行评估。