CS-003 is a potent triple neurokinin receptor antagonist, targeting NK1, NK2, and NK3 receptors with Ki values of 2.3 nM, 0.54 nM, and 0.74 nM, respectively, in human tissues. It demonstrates superior inhibitory activity against guinea pig neurokinin receptors as well, with Ki values of 5.2 nM, 0.47 nM, and 0.71 nM. CS-003 significantly inhibits inositol phosphate formation related to the neurokinin signaling of substance P, neurokinin A, and neurokinin B. Furthermore, it effectively reduces citric acid-induced cough, exhibiting enhanced activity compared to selective neurokinin receptor antagonists, making it valuable for research in neurogenic respiratory disorders.
CS-003 is a potent triple neurokinin receptor antagonist, targeting NK1, NK2, and NK3 receptors with Ki values of 2.3 nM, 0.54 nM, and 0.74 nM, respectively, in human tissues. It demonstrates superior inhibitory activity against guinea pig neurokinin receptors as well, with Ki values of 5.2 nM, 0.47 nM, and 0.71 nM. CS-003 significantly inhibits inositol phosphate formation related to the neurokinin signaling of substance P, neurokinin A, and neurokinin B. Furthermore, it effectively reduces citric acid-induced cough, exhibiting enhanced activity compared to selective neurokinin receptor antagonists, making it valuable for research in neurogenic respiratory disorders.
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