Haye-Legrand I, Cerrina J, Raffestin B, Labat C, Boullet C, Bayol A, Benveniste J, Brink C
J Pharmacol Exp Ther. 1986 Nov;239(2):536-41.
Histamine concentration-effect curves were obtained using either an individual or cumulative dosing method. The maximal response to histamine in bronchial preparations using the individual dosing protocol was 0.25 +/- 0.03 g/mm2 and similar results were obtained using the cumulative method (0.24 +/- 0.03 g/mm2). The sensitivity (pD2 value) of isolated human bronchial muscle preparations was comparable for both the individual and cumulative methods (5.71 and 5.16, respectively). Prostaglandin (PG) E2 and PGF2 alpha contracted isolated human bronchial muscle preparations and the pD2 values were 5.64 and 5.59, respectively. PGE2 did not relax bronchial muscle preparations contracted with histamine (50 microM). At high concentrations prostacyclin (3 microM) relaxed histamine-contracted bronchial tissues but this effect was quite variable. Indomethacin (1.7 microM) did not affect basal tone in bronchial tissues. Isolated human bronchial preparations which were contracted maximally with histamine always released measurable quantities of PGs. In some experiments the rat stomach strip was used to detect the presence of these substances before and subsequent to the indomethacin (1.7 microM) treatment. The use of radioimmunoassay for PGE2 and PGF2 alpha confirmed these bioassay results. In a large number of experiments (18 preparations from 9 individual lung samples) the baseline production of PGs was PGE2, 22.9 +/- 2.8 pg/mg of tissue and PGF2 alpha, 11.9 +/- 2.5 pg/mg of tissue. Subsequent to histamine stimulation the quantities of PGs released were PGE2, 72.4 +/- 7.6 pg/mg of tissue and PGF2 alpha, 40.9 +/- 7.3 pg/mg of tissue.(ABSTRACT TRUNCATED AT 250 WORDS)
使用个体给药或累积给药方法获得组胺浓度 - 效应曲线。采用个体给药方案时,支气管制剂对组胺的最大反应为0.25±0.03 g/mm²,采用累积给药方法也得到了类似结果(0.24±0.03 g/mm²)。个体给药和累积给药方法中,分离的人支气管肌肉制剂的敏感性(pD2值)相当(分别为5.71和5.16)。前列腺素(PG)E2和PGF2α使分离的人支气管肌肉制剂收缩,pD2值分别为5.64和5.59。PGE2不能使由组胺(50μM)收缩的支气管肌肉制剂舒张。高浓度时(3μM)前列环素可使组胺收缩的支气管组织舒张,但这种效应变化较大。吲哚美辛(1.7μM)不影响支气管组织的基础张力。用组胺最大程度收缩的分离人支气管制剂总是能释放出可测量量的PGs。在一些实验中,在吲哚美辛(1.7μM)处理之前和之后,用大鼠胃条检测这些物质的存在。用放射免疫分析法检测PGE2和PGF2α证实了这些生物测定结果。在大量实验中(来自9个个体肺样本的18个制剂),PGs的基础产量为:PGE2,22.9±2.8 pg/mg组织;PGF2α,11.9±2.5 pg/mg组织。组胺刺激后,释放的PGs量为:PGE2,72.4±7.6 pg/mg组织;PGF2α,40.9±7.3 pg/mg组织。(摘要截短至250字)