Description
Pranlukast, a novel chromone derivative, was introduced in Japan for
the treatment of bronchial asthma and allergic diseases. Pranlukast is a highly potent,
selective and competitive antagonist of peptidoleukotrienes with high affinity for the
LTD4 receptor. In patients with bronchial asthma, pranlukast was reported to induce
significant improvement in both immediate and late asthmatic response induced by
antigen. Pranlukast is also being evaluated clinically for the treatment of perennial
allergic rhinitis, pediatric asthma, and cutaneous pruritus in dialysis patients. The
therapeutic potential of pranlukast in managing irritable bowel syndrome has been
suggested.
Chemical Properties
Off-white solid
Uses
A potent, selective and orally active CysLT receptor antagonist. Leukotriene antagonist. Used as an antiasthmatic
Uses
antiasthmatic;leukotriene receptor-1 antagonist
Uses
Labeled Pranlukast, intended for use as an internal standard for the quantification of Pranlukast by GC- or LC-mass spectrometry.
Definition
ChEBI: N-[4-oxo-2-(2H-tetrazol-5-yl)-1-benzopyran-8-yl]-4-(4-phenylbutoxy)benzamide is a member of chromones.
Biological Activity
Selective cysteinyl leukotriene receptor 1 (CysLT 1 ) antagonist (IC 50 values are ~ 4-7 and 3620 nM for CysLT 1 and CysLT 2 respectively). Inhibits contraction of airway smooth muscle, microvascular leakage into airways and eosinophil infiltration. Can decrease symptoms of bronchial asthma.
References
1) Nakai?et al. (1988),?New Potent Antagonists of Leukotrienes C4 and D4. 1. Synthesis and Structure-Activity Relationships; J. Med. Chem.?31?84
2) Taniguchi?et al.?(1993),?The effect of an oral leukotriene antagonist, ONO-1078, on allergen-induced immediate bronchoconstriction in asthmatic subjects; J. Allergy Clin. Immunol.?92?507
3) Ciana?et al.?(2006),?The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptor; EMBO J.?25?4615
4) Hennen?et al. (2013),?Decoding Signaling and Function of the Orphan G Protein-Coupled Receptor GPR17 with a Small-Molecule Agonist; Sci. Signal.?6?ra93
