L-R4W2 acetate is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1 ), with an IC50 of 0.1 μM. L-R4W2 acetate may act as a potent analgesic [1] [2].
References:
[1]. Planells-Cases R, et, al. Arginine-rich peptides are blockers of VR-1 channels with analgesic activity. FEBS Lett. 2000 Sep 15; 481(2): 131-6.
[2]. Himmel HM, et, al. The arginine-rich hexapeptide R4W2 is a stereoselective antagonist at the vanilloid receptor 1: a Ca2+ imaging study in adult rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 2002 Jun; 301(3): 981-6.
References:
[1]. Planells-Cases R, et, al. Arginine-rich peptides are blockers of VR-1 channels with analgesic activity. FEBS Lett. 2000 Sep 15; 481(2): 131-6.
[2]. Himmel HM, et, al. The arginine-rich hexapeptide R4W2 is a stereoselective antagonist at the vanilloid receptor 1: a Ca2+ imaging study in adult rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 2002 Jun; 301(3): 981-6.