TRPV1 antagonist 9 (compound 13c) is an orally active transient receptor potential vanilloid 1 ( TRPV1 ) channel antagonist. TRPV1 antagonist 9 blocks Ca 2+ uptake by CHO cells expressing TRPV1 receptors with IC 50 values are 0.6 and 0.8 nM for Capsaicin ( HY-10448 ) and acid-induced Ca 2+ uptake, respectively. TRPV1 antagonist 9 blocks Capsaicin ( HY-10448 )-induced flinch response and causes hyperthermia in rats.
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