目的：比较RR-福莫特罗和rac-福莫特罗对人支气管舒张作用。方法：将内径2～4mm、长15mm的人支气管螺旋条置入持续供氧的浴槽内，静息张力为1g，以蓄积给药法测定RR-福莫特罗（10 pmol•L-1～3.2 Lmol•L-1）和rac-福莫特罗（10 pmol•L-1～3.2 Lmol•L-1）在静息情况下，及氨甲酰胆碱（10 Lmo l•L-1）或组胺（100 Lmol•L-1）引起收缩情况下的张力改变。结果：RR-福莫特罗在静息状况下支气管舒张作用强于rac-福莫特罗（P<0.05）。RR-福莫特罗和rac-福莫特罗对抗由氨甲酰胆碱和组胺引起的收缩，且RR-福莫特罗的对抗作用强于rac-福莫特罗（P<0.05）。结论：RR-福莫特罗对人支气管的舒张作用强于rac-福莫特罗。

To study the inductive expression of human phosphodiesterase 4A (hPDE4A) in yeast cell GL62 and investigate the inhibitory effects of theophylline, rolipram, and acetamide-45 on PDE4A activity of the expressed product in yeast cell GL62. METHODS: Yeast cell GL62 were transfected with human PDE4A gene cloned in the expression plasmid p138NB. Expression was induced by adding CuSO4 to a final concentration of 150μmol/L, and the expressed product was extracted. The activity of PDE4A was detected by HPLC. RESULTS: Yeast cell GL62 expressed a certain protein at CuSO4 150μmol/L, the size of the expressed product was between 62 kDa and 83 kDa, the activity of PDE4A of the expressed product at 3 h was in maximum (188±23)μmol×g-1×min-1, and the Km was (17.7±2.6) mmol/L. Theophylline, rolipram, and acetamide-45 could inhibit the activity of PDE4A extracted from yeast cell GL62. The IC50 (95% confidence limits) of theophylline, rolipram, and acetamide-45 were 1642 (989-2727), 4.58 (3.45-6.08), and 275 (170-444) mmol/L respectively. CONCLUSION: PDE4A expressed in yeast cell GL62 is biologically active. Theophylline, rolipram, and acetamide-45 can inhibit the PDE4A activity. The expressed product in yeast cell GL62 may be used in the research work of PDE4 and its inhibitors.

To compare the bronchodilating and antiinflammatory effects of oral racemic formoterol (rac-FMT) and (R,R)-formoterol (R,R-FMT). METHODS: The changes of lung resistance (RL), dynamic lung compliance (Cdyn), and the accumulation of inflammatory cells in bronchoalveolar lavage fluids (BALF) induced by ovalbumin aerosol in sensitized guinea pigs and mice were investigated in vivo. RESULTS: Mean value increase of RL and mean value reduction of Cdyn from 1 to 30 min after antigen challenge were up to 101%

To explore the changes of leukotrienes (LT) in cerebral cortex and lung tissues in ovalbumin-induced rat asthma model and effects of different anti-asthma drugs on the changes. METHODS: Aerosol antigen-induced changes of inflammation in bronchoalveolar lavage fluids (BALF), pulmonary and brain histologic section in sensitized rats were investigated. Changes of LTB4 and LTC4 in lung and cerebral cortex homogenates were analyzed by reverse-phase high performance liquid chromatography (RP-HPLC). RESULTS: The number of inflammatory cells in BALF and the score of lung and brain histological examination from antigen- challenged rats were significantly higher than that from control group (P<0.05). Dexamethason (DXM, 0.5mg/kg, ip) and ketotifen fumarate (KF, 5mg/kg, ig) markedly reduced total leukocyte number in BALF, and inhibited eosinophil accumulation, reduced the infiltration of eosinophils, and improved mucous edema and epithelial lesion of bronchi and bronchioles. In addition, RP-HPLC results shown LTB4 in lung and cerebral cortex homogenates were increased in antigenchallenged rats [(4.1

研究VLA24 拮抗剂BIO-1211对嗜酸粒细胞趋化、聚集和释放的影响。方法：采用离体方法测定血小板活化因子（PAF） 诱导的嗜酸性粒细胞反应，整体方法观察嗜酸性粒细胞聚集和释放反应。结果：BIO-1211能明显抑制PAF对嗜酸性粒细胞的趋化作用，BIO-12114×10-11、4×10-10、4×10-9 mol·L-1的抑制率分别为2419%、2919%、3113%。BIO-12111、3、10mg·kg- 1单次腹腔给药，呈剂量依赖性抑制大鼠葡聚糖凝胶引起的腹腔嗜酸粒细胞聚集，抑制率分别为013%、6819% 和7219% （P<0105），但不能抑制嗜酸性粒细胞释放嗜酸细胞过氧化物酶。结论：BIO-1211抑制嗜酸性粒细胞趋化和聚集, 减轻局部炎症反应, 有可能发展成为一种新的抗变态反应性药物。