JNJ-17203212

JNJ-17203212 is a reversible and potent antagonist of transient receptor potential vanilloid 1 (TRPV1) with pKi values of 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively. It Inhibits capsaicin- and low pH- induced channel activation with pIC₅₀ values of 6.32 and 7.23 respectively. Intraperitoneal administration of JNJ17203212 (20 mg/kg) attenuates capsaicin evoked coughs. Chronic administration of JNJ-17203212 (30 mg/kg, s.c., twice daily) shows analgesic activity in an in vivo model of bone cancer pain.