SB-366791

The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin. TRPV1 is present in primary sensory neurons and in both central and peripheral sensory nerve terminals and plays a role in thermal and mechanical hyperalgesia. SB-366791 is a selective TRPV1 antagonist that is widely used in pain research.¹ In cultured trigeminal ganglion neurons, SB-366791 inhibits capsaicin-evoked Ca²⁺ influx with an IC₅₀ value of 0.7 μM.¹ A 1 nmol injection of SB-366791 in mouse paw reduces capsaicin-induced nociceptive responses in a model of pain.² Intrathecal pretreatment of 10 μl SB-366791 in rats suppresses tolerance to the analgesic effects of chronic morphine administration.³ Co-administration of morphine and SB-366791 at 0.1 mg/kg has potent analgesic effects in a mouse model of bone cancer pain.⁴

WARNING This product is not for human or veterinary use.

1. Varga, A., Németh, J., Szabó, A., et al. Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat. Neurosci. Lett. 385(2), 137-142 (2005).

2. Andrade, E.L., Luiz, A.P., Ferreira, J., et al. Pronociceptive response elicited by TRPA1 receptor activation in mice. Neuroscience 152(2), 511-520 (2008).

3. Chen, Y., Geis, C., and Sommer, C. Activation of TRPV1 contributes to morphine tolerance: Involvement of the mitogen-activated protein kinase signaling pathway. J. Neurosci. 28(22), 5836-5845 (2008).

4. Niiyama, Y., Kawamata, T., Yamamoto, J., et al. SB366791, a TRPV1 antagonist, potentiates analgesic effects of systemic morphine in a murine model of bone cancer pain. Br. J. Anaesth. 102(2), 251-258 (2009).