1.Protective effect of a new anti-asthmatic agent (Minocromil) in bronchial allergen challenge tests.
Svendsen UG, Frølund L, Madsen F, Weeke B. Allergy. 1985 Aug;40(6):458-60.
Ten patients were included in a double-blind crossover trial, designed to compare the effects of a new anti-asthmatic agent Minocromil, an organic decarboxylic acid, and placebo on bronchial allergen challenge. The challenges were performed at weekly intervals. Significant differences in favour of Minocromil were found in the concentration of antigen reached at which FEV1 fell below 20% of baseline. This was confirmed by analysis of the decrease in FEV1 recorded at the highest concentrations of antigens, which showed statistically significant differences in favour of Minocromil.
2.New antiallergic pyrano [3,2-g]quinoline-2,8-dicarboxylic acids with potential for the topical treatment of asthma.
Cairns H, Cox D, Gould KJ, Ingall AH, Suschitzky JL. J Med Chem. 1985 Dec;28(12):1832-42.
A number of antiallergic pyranquinolinedicarboxylic acid derivatives with potential for the topical treatment of asthma have been synthesized. All the compounds have been evaluated against rat passive cutaneous anaphylaxis and in a dog hypotension screen. This is the first detailed description of the application of the latter screen for the identification of antiallergic agents. Two compounds, disodium 9-ethyl-6, 9-dihydro-4,6-dioxo-10-propyl-4H-pyrano [3,2-g]quinoline-2,8-dicarboxylate (86) and disodium 6-(methylamino)-4-oxo-10-propyl-4H-pyrano[3,2-g]-quinoline-2, 8-dicarboxylate (72), were selected and further evaluated for their ability to induce phosphorylation of a 78000 molecular weight protein associated with the rat peritoneal mast cell. Their ability to inhibit histamine release from these cells and from a mucosal mast cell preparation has also been evaluated. These compounds, nedocromil sodium (TILADE 86) and minocromil (the free acid of 72), are at present undergoing therapeutic evaluation.
3.Attenuation of exercise-induced asthma by pretreatment with nedocromil sodium and minocromil.
Roberts JA, Thomson NC. Clin Allergy. 1985 Jul;15(4):377-81.
In a group of atopic adult asthmatic patients the effects of two new inhaled antiasthmatic drugs, nedocromil sodium and minocromil were studied in two independent randomized double-blind trials to assess their efficacy in preventing exercise-induced asthma (EIA). Exercise testing consisted of steady state running on an inclined treadmill. Neither drug administered 30 min before exercise significantly altered baseline FEV1. Nedocromil sodium (2 and 4 mg) pre-treatment in nine patients and minocromil (4 mg) in eight patients gave significant protection (P less than 0.001) compared to placebo as assessed by the reduction in the maximum percentage fall in FEV1. There was no significant difference in the inhibitory effect of the two doses of nedocromil sodium. These results indicate that both nedocromil sodium and minocromil can attenuate EIA.