ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with K i values of 0.12 nM for NK1 and 0.62 nM for NK2 . At a concentration of 100 nM, ZD6021 has a pK B value of 8.9 for human pulmonary artery NK1 receptors, and a pK B value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED 50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED 50 of 13 mg/kg.
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