Prevention of Histamine Release

The release of histamine in vitro may be prevented by the aid of certain medicinally acive compounds. Such substances are not usually absorbed by the gastro-intestinal tract. An attempt has been made to find a similar substance which might be absorbed when administered orally and whieh possesses anti-allergic properties. Two such compoimds are disucssed below namely Sodinm cromoglycate and Ketotifen fumarate. 

Sodium Cromoglycate BAN, Cromolyn Sodium USAN, Cromoglicic Acid INN 

Sodium cromoglycate is a chromono derivative whieh inhibits the release of histamine and SRS-A in allergic reactions. It is mostly employed in the prophylactic treatment of asthma. It is administered only by inhalation, either alone or in conjimetion with a small quantity of isoprenaline to prevent bronehospasm caused by the inhalation of the fine powder. 

9-Dihydro-4-(l-methyl-4-piperidylidene)-10H-benzo [4, 5] cyclohepta [1, 2-Z ] thiophen-10- 

It possesses anti-allergic properties similar to those of sodium cromoglycate and is used in the prophylactic treatment of asthma. 

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Nedocromil, 9-Etkyl-6,tFdihydrO-4,6 ioxo-IO-propyl-4H-pyrano[3,2-g]qu i notine-2, H-dicarboxylic acid 4,6-dioxo-1 -ethyl-10-propyl-4H,6H-pyrano[3,2-g]quinotlne-2,8-dicar boxy lie acid FPL 59002. C HpNO, mol wt 371.35. C 61.45%, H 4.61%, N 3.77%, O 30.16%. Anti-aller-gic compound with the ability to stabilize both mucosal and connective tissue mast cells. Prepn and pharmacology H. Cairns, D. Cox. Belg. pat. 866,622 eidem, U.S. pat. 4,474,-787 (1978, 1984 both to Fisons) H. Cairns et at, J. Med. Chem. 28, 1832 (1985). Prevention of histamine release from mast celts, inhibition of Monchoconstriction in monkeys R. P. Eady et at.. Bril. J. Pharmacol 85, 323 (1985). Early clinical trial in bronchial asthma S. Lai et al. Thorax 39, 809 (1984). 

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