JYL1421 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).1 It inhibits calcium uptake induced by capsaicin in CHO cells expressing rat TRPV1 (EC50 = 9.2 nM). JYL1421 inhibits capsaicin-induced release of the neuropeptides somatostatin, substance P , and calcitonin gene-related peptide (CGRP) from isolated rat trachea (IC50s = 227-491 nM).2 It inhibits capsaicin-induced hypothermia and hypotension in rats when administered at doses of 2 and 0.4 mg/kg, respectively. JYL1421 (2 mg/kg) also reduces the number of wiping movements induced by ocular administration of capsaicin in rats. Unlike several other TRPV1 antagonists, JYL1421 does not induce hyperthermia in rats when administered at doses ranging from 1.02 to 32.77 μmol/kg.3
1.Wang, Y., Szabo, T., Welter, J.D., et al.High affinity antagonists of the vanilloid receptorMol. Pharmacol.62(4)947-956(2002) 2.Jakab, B., Helyes, Z., Varga, A., et al.Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the ratEur. J. Pharmacol.517(1-2)35-44(2005) 3.Garami, A., Shimansky, Y.P., Pakai, E., et al.Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermiaJ. Neurosci.30(4)1435-1440(2010)