Transient receptor potential vanilloid type 1 (TRPV1) is a member of the transient receptor potential (TRP) family that is activated or sensitized by a variety of endogenous stimuli as a result of tissue injury and inflammation. TRPV1 is upregulated during inflammation and plays a role in the perception of pain.^1,2 Capsazepine is a competitive antagonist of TRPV1 which blocks the capsaicin-induced uptake of Ca2+ in neonatal rat dorsal root ganglia with an IC₅₀ of 0.42 µM and Chinese hamster ovary cells with an IC₅₀ of 17 nM.^1,3 It does not block acid- or heat-induced activation of TRPV1 and may block receptors other than TRPV1.^4,5

1 Doherty, E.M., Fotsch, C., Bo, Y., et al. Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J Med Chem 48 71-90 (2005).

2 Walker, K.M., Urban, L., Medhurst, S.J., et al. The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain. J Pharmacol Exp Ther 304(1) 56-60 (2003).

3 Walpole, S.J., Bevan, S., Bovermann, G., et al. The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin. J Med Chem 37 1942-1954 (1994 Feb 2).

4 Liu, L., Simon, S.A. Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia. Neurosci Lett 228 29-32 (1997).

5 Docherty, R.J., Yeats, J.C., Piper, A.S. Capsazepine block of voltage-activated calcium channels in adult rat dorsal root ganglion neurones in culture. Br J Pharmacol 121 1461-1467 (1997).

Doherty, E.M., Fotsch, C., Bo, Y., et al. Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J Med Chem 48 71-90 (2005).

Walker, K.M., Urban, L., Medhurst, S.J., et al. The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain. J Pharmacol Exp Ther 304(1) 56-60 (2003).

Liu, L., Simon, S.A. Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia. Neurosci Lett 228 29-32 (1997).

Walpole, S.J., Bevan, S., Bovermann, G., et al. The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin. J Med Chem 37 1942-1954 (1994 Feb 2).

Chan, H.E.H., Jilani, I., Chang, R., et al. Cell-free bead-based detection of total and phosphorylated proteins in plasma and cell lysates: Detection of FLT3. (2007).

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Capsazepine is available in the following screening library:

• Bio-active Lipid I Screening Library (96-Well)