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.
IC50 & Target[1][2]
hTRPV1 2.66 nM (IC50) TRPM8 7.45 μM (IC
体外研究(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) . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel.
TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats.
TRPV1 antagonist 3 (10 mg/kg; i.v.) shows a good concentration in the brain at 0.5 h, with value of 2311 ng/g, and has good CNS penetration, with a brain/plasma ratio of 1.66. has not independently confirmed the accuracy of these methods. They are for reference only.