Senktide (trifluoroacetate salt)

Senktide is a potent, selective agonist of the neuromedin K3 (NK₃) receptor (EC₅₀ = 0.5-3 nM).^1,2,3 It less potently agonizes the NK₁ receptor (EC₅₀ = 35 µM) and is without effect on the NK₂ receptor.^1,2,3 Senktide is used to study the action of the NK₃ receptor in cells and in animals.^4,5

1.Byk, G., Halle, D., Zeltser, I., et al.Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance PJ. Med. Chem39(16)3174-3178(1996) 2.Sarau, H.M., Griswold, D.E., Potts, W., et al.Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonistJ. Pharmacol. Exp. Ther.281(3)1303-1311(1997) 3.Harrison, T., Korsgaard, M.P., Swain, C.J., et al.High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural templateBioorg. Med. Chem. Lett.8(11)1343-1348(1998) 4.Thakar, A., Sylar, E., and Flynn, F.W.Activation of tachykinin, neurokinin 3 receptors affects chromatin structure and gene expression by means of histone acetylationPeptides38(2)282-290(2012) 5.Gaskins, G.T., Glanowska, K.M., and Moenter, S.M.Activation of neurokinin 3 receptors stimulates GnRH release in a location-dependent but kisspeptin-independent manner in adult miceEndocrinology154(11)3984-3989(2013)