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TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC 50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
Appearance:Solid
IC50& Target:hTRPV1 2.66 nM (IC 50 ) TRPM8 7.45 μM (IC 50 )
In Vitro:TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels. TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL). MCE has not independently confirmed the accurac
In Vivo:TRPV1 antagonist 3 (Compound 7q) (0-30mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel. TRPV1 antagonist 3 (0-100mg/kg; i.g.) had no obvious thermal effect in rats. TRPV1 antagonist 3 (10 mg/
Biological Activity:TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC 50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.