Leukotriene LTD4 receptor antagonist

Leukotriene D4 (LTD4) is formed from the metabolism of arachidonic acid by 5 -lypoxygenase and is considered to be an important receptor-mediator of human bronchial asthma. As a consequence, specific leucotriene LTD4 receptor antagonists are potential therapeutics for the treatment of asthma. The... 

FIGURE 9.20 Design of multiple ligancl activity, (a) Dual histamine HI receptor and leukotriene receptor antagonist incorporating known antihistaminic properties of cyproheptadine and LTD4. (b) Joint ACE/NEP inhibitor formed from incorporating similarities in substrate structures for both enzymes. From [57],... 

LTC4 and LTD4 are potent bronchoconstrictors and are recognized as the primary components of the slow-reacting substance of anaphylaxis (SRS-A) that is secreted in asthma and anaphylaxis. There are four current approaches to antileukotriene drug development 5-LOX enzyme inhibitors, leukotriene-receptor antagonists, inhibitors of FLAP, and phospholipase A2 inhibitors. 

Cysteinyl leukotrienes interact with two classes of receptors, termed cys-LT, (formerly LTD4 receptors) and cys-LTj (formerly LTC4 receptors) as determined by their order of potency in bioassays and their characteristics in receptor binding assays in mammalian tissues and cells (see [18] for review). While cys-LT, receptors are well characterized owing to the availability of antagonists, cys-LTj receptors are... 

Leukotriene D4 Receptor (LTD4), CysLT-1 Receptor Antagonists... 

Biological target Montelukast is a 7-chloroquinolme-substituted derivative of the leukotriene D4 (LTD4) molecule and a seccaid generation antagonist at the CysLT-1 receptor for LTD4, a bronchoconstrictor mediator in allergic inflammation. 

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