Pranlukast (103177-37-3)is a selective Leukotriene CysLT1 antagonist1 and has been used in the treatment of asthma2. Pranlukast is also an inhibitor of GPR173 (IC50’s = 10.5nM hGPR17, 31nM rGPR17) and is superior to Montelukast in achieving functional inhibition4.
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