LIPID MAPS

Capsaicin is a terpene alkaloid that has been found in Capsicum and has diverse biological activities.^1,2,3,4 It induces inward currents in HEK293 cells expressing rat transient receptor potential vanilloid 1 (TRPV1; EC50 = 0.64 µM at neutral pH), an effect that can be blocked by the TRPV1 inhibitor A-425619.1 Capsaicin (10 and 50 µM) decreases LPS-induced prostaglandin E2 (PGE2) production, as well as reduces LPS- and IFN-induced nitric oxide (NO) release in isolated mouse peritoneal macrophages.² Capsaicin induces substance P release in rat spinal cord slices with an EC50 value of 2.3 µM.³ It reduces acetylcholine- or phenylquinone-induced writhing (ED50s = 1.33 and 1.38 mg/kg, respectively, s.c.) but has no effect on the latency to paw withdrawal in the hot plate test in mice (ED50 = >20 mg/kg, s.c.).⁴ Formulations containing capsaicin have been used in the treatment of nerve pain associated with shingles.

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References

1. Neelands, T.R., Jarvis, M.F., Han, P., et al. Acidification of rat TRPVI alters the kinetics of capsaicin responses. Mol. Pain 1, 28 (2005).

2. Kim, C.-S., Kawada, T., Kim, B.-S., et al. Capsaicin exhibits anti-inflammatory property by inhibiting IkB-a degradation in LPS-stimulated peritoneal macrophages. Cell. Signal. 15(3), 299-306 (2003).

3. Marvizón, J.C.G., Wang, X., Matsuka, Y., et al. Relationship between capsaicin-evoked substance P release and neurokinin 1 receptor internalization in the rat spinal cord. Neuroscience 118(2), 535-545 (2003).

4. Hayes, A.G., Skingle, M., and Tyers, M.B. Effects of single doses of capsaicin on nociceptive thresholds in the rodent. Neuropharmacology 20(5), 505-511 (1981).