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.
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See how others have used Capsazepine. Click on the entry to view the PubMed entry .
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