Capsazepine

Capsazepine is a competitive antagonist of the VR1 (TRPV1, also transient receptor potential vanilloid type 1), antagonizing the effects produced by Capsaicin at this receptor (sc-3577). The VR1 (TRPV1 receptor) is a non-selective ligand-gated cation channel that responds to noxious heat, protons, and Capsaicin, producing nociception signals. Capsazepine also activates ENaCδ (amiloride-sensitive epithelial Na+ channel). Capsazepine is shown to inhibit the development of mechanical hyperalgesia induced by intraplanar capsaicin injection. Capsazepine is described to block Resiniferatoxin (sc-24015)- and Capsaicin-induced contractions of guinea pig treacheal smooth muscle. Studies investigating the function of the VR1 (TRPV1 receptor) have employed Capsazepine as a tool for perturbing systemic neuronal response to Capsaicin. 参考文献 1. Urban, L. and Dray, A. 1991. Neurosci. Lett. 134: 9-11. PMID: 1726117 2. Bevan, S., et al. 1992. Br. J. Pharmacol. 107: 544-552. PMID: 1422598 3. Maggi, C.A., et al. 1993. Br. J. Pharmacol. 108: 801-805. PMID: 7682139 4. Walpole, C.S., et al. 1994. J. Med. Chem. 37: 1942-1954. PMID: 8027976 5. Ellis, J.L. and Undem, B.J. 1994. J. Pharmacol. Exp. Ther. 268: 85-89. PMID: 8301598 6. Liu, L. and Simon, S.A. 1997. Neurosci. Lett. 228: 29-32. PMID: 9197280 7. Walker, K.M., et al. 2003. J. Pharmacol. Exp. Ther. 304: 56-62. PMID: 12490575 8. Valenzano, K.J. and Sun, Q. 2004. Curr. Med. Chem. 11: 3185-3202. PMID: 15579007

376.90

Capsazepine is an antagonist of TRPV1 and activator of ENaC

N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide

C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O

C19H21ClN2O2S

138977-28-3