ZD6021 is a potent antagonist of the Neurokinin 1 (NK1) receptor, exhibiting a Ki value of 0.12 nM for NK1 and 0.62 nM for NK2. This compound has demonstrated significant biological activity by reducing plasma protein extravasation in guinea pigs induced by ASMSP, with an effective dose (ED50) of 0.5 mg/kg. Additionally, ZD6021 effectively mitigates NK2-mediated bronchoconstriction, showcasing an ED50 of 13 mg/kg. Its selective antagonism supports research applications in understanding neurogenic inflammation and respiratory conditions.
ZD6021 is a potent antagonist of the Neurokinin 1 (NK1) receptor, exhibiting a Ki value of 0.12 nM for NK1 and 0.62 nM for NK2. This compound has demonstrated significant biological activity by reducing plasma protein extravasation in guinea pigs induced by ASMSP, with an effective dose (ED50) of 0.5 mg/kg. Additionally, ZD6021 effectively mitigates NK2-mediated bronchoconstriction, showcasing an ED50 of 13 mg/kg. Its selective antagonism supports research applications in understanding neurogenic inflammation and respiratory conditions.
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